COVID-19
阻害剤の選択性比較
カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
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水 | DMSO | アルコール | ||
S2853 | Carfilzomib (PR-171) | <1 mg/mL | 50 mg/mL | <1 mg/mL |
S1185 | Ritonavir | <1 mg/mL | 100 mg/mL | 3 mg/mL |
S1538 | Telaprevir (VX-950) | <1 mg/mL | 136 mg/mL | <1 mg/mL |
S1380 | Lopinavir | <1 mg/mL | 126 mg/mL | 126 mg/mL |
S1322 | Dexamethasone | <1 mg/mL | 79 mg/mL | 6 mg/mL |
S0833 | EIDD-1931 | 15 mg/mL | -1 mg/mL | 3 mg/mL |
S8969 | Molnupiravir (EIDD-2801) | 20 mg/mL | 66 mg/mL | '22 mg/mL |
S8932 | Remdesivir (GS-5734) | <1 mg/mL | 100 mg/mL | '''16 mg/mL |
S6676 | Ebselen | <1 mg/mL | 55 mg/mL | <1 mg/mL |
S2169 | Rosuvastatin Calcium | <1 mg/mL | 100 mg/mL | <1 mg/mL |
S1183 | Danoprevir (ITMN-191) | <1 mg/mL | 144 mg/mL | 144 mg/mL |
S2851 | Baricitinib (INCB028050) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
S2485 | Mitoxantrone 2HCl | 89 mg/mL | 89 mg/mL | <1 mg/mL |
S1759 | Pitavastatin Calcium | <1 mg/mL | 51 mg/mL | <1 mg/mL |
S1401 | Tenofovir | 2 mg/mL | 4 mg/mL | <1 mg/mL |
S2823 | Tideglusib | <1 mg/mL | 8 mg/mL | <1 mg/mL |
S3035 | Daunorubicin HCl | 100 mg/mL | 100 mg/mL | <1 mg/mL |
S1386 | Nafamostat Mesylate | 53 mg/mL | 20 mg/mL | <1 mg/mL |
S1680 | Disulfiram | <1 mg/mL | 59 mg/mL | '59 mg/mL |
S1706 | Lamivudine | 46 mg/mL | 46 mg/mL | <1 mg/mL |
S1620 | Darunavir Ethanolate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
S4157 | Chloroquine diphosphate | 100 mg/mL | <1 mg/mL | <1 mg/mL |
S1351 | Ivermectin | <1 mg/mL | 100 mg/mL | 28 mg/mL |
S1289 | Carmofur | <1 mg/mL | 52 mg/mL | 10 mg/mL |
S4028 | Dexamethasone Sodium Phosphate | 103 mg/mL | <1 mg/mL | <1 mg/mL |
S1835 | Azithromycin | <1 mg/mL | 100 mg/mL | 100 mg/mL |
S3037 | Bepotastine Besilate | <1 mg/mL | 109 mg/mL | <1 mg/mL |
S2874 | Camostat Mesilate | 10 mg/mL | 99 mg/mL | <1 mg/mL |
S3124 | Dexamethasone Acetate | <1 mg/mL | 87 mg/mL | 20 mg/mL |
S3079 | Atovaquone | <1 mg/mL | 5 mg/mL | <1 mg/mL |
S2079 | Moexipril HCl | <1 mg/mL | 20 mg/mL | <1 mg/mL |
S1691 | Praziquantel | <1 mg/mL | 63 mg/mL | 63 mg/mL |
S2926 | TDZD-8 | <1 mg/mL | 44.5 mg/mL | 44.5 mg/mL |
S7393 | Aloxistatin(E64d) | <1 mg/mL | 68 mg/mL | 68 mg/mL |
S8279 | Shikonin | <1 mg/mL | 57 mg/mL | 23 mg/mL |
S7975 | Favipiravir (T-705) | 5 mg/mL | 31 mg/mL | 22 mg/mL |
S5250 | Darunavir | <1 mg/mL | 100 mg/mL | 11 mg/mL |
S5754 | Baricitinib phosphate | -1 mg/mL | 94 mg/mL | -1 mg/mL |
S7392 | Loxistatin Acid (E-64C) | 2 mg/mL | 62 mg/mL | '62 mg/mL |
S7262 | Vidofludimus | <1 mg/mL | 100 mg/mL | 1 mg/mL |
S7947 | PX-12 | <1 mg/mL | 38 mg/mL | 38 mg/mL |
S5911 | Bictegravir | <1 mg/mL | 90 mg/mL | <1 mg/mL |
S4646 | Ciclesonide | <1 mg/mL | 100 mg/mL | ''100 mg/mL |
S4430 | Hydroxychloroquine Sulfate | 67 mg/mL | <1 mg/mL | <1 mg/mL |
S7579 | Ledipasvir (GS5885) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
S9567 | Indinavir Sulfate | -1 mg/mL | 100 mg/mL | -1 mg/mL |
S3724 | Velpatasvir | 100 mg/mL | 100 mg/mL | 100 mg/mL |
S3733 | Boceprevir | <1 mg/mL | 100 mg/mL | 100 mg/mL |
S2071 | Prulifloxacin (NM441) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
S4282 | Nelfinavir Mesylate | <1 mg/mL | 100 mg/mL | '100 mg/mL |
COVID-19製品
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S2853 |
Carfilzomib (PR-171)Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis. |
![]() ![]() Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,
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S1185 |
RitonavirRitonavir (ABT-538, A 84538) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis. |
![]() ![]() (A) KMS11 and
(B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown).
(C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to
untreated cells (not shown).
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S1538 |
Telaprevir (VX-950)Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
![]() ![]() HCV replicon genotype 1b cells were passaged in the presence of G418 alone (medium 694 control) or G418 with miravirsen, SPC4729 (oligonucleotide negative control) or telaprevir for 28 days in fixed concentrations at a multiple (X) of the EC50 of miravirsen or telaprevir. Colony formation was assessed by staining surviving cells with crystal violet.
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S1380 |
LopinavirLopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
![]() ![]() Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
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S1322 |
DexamethasoneDexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S0833新 |
EIDD-1931EIDD-1931 (NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
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S8969新 |
Molnupiravir (EIDD-2801)Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
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S8932新 |
Remdesivir (GS-5734)Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
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S6676新 |
EbselenEbselen (DR 3305, SPI-1005, PZ-51) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. |
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S2169 |
Rosuvastatin CalciumRosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay. |
![]() ![]() MDA-MB-231 cells were treated with simvastatin (SIM) or rosuvastatin (ROSU) in combination with ZOL for 48 h. Vitality and apoptosis were measured by using the cell titer blue and the caspase 3/7 Glo assay. Data are shown as mean ± SD of at least three individual experiments (*p ≤ 0.05; **p ≤ 0.01; ***p ≤ 0.001). |
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S1183 |
Danoprevir (ITMN-191)Danoprevir (ITMN-191, RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2. |
![]() ![]() Western blot analysis of HCV NS3 protease cleavage of MAVS. The catalytic efficiency of four proteases (H, H-A156T, 41 and 41-A156T) from individuals H and 41 were tested in the absence or presence of an NS3 protease inhibitor (danoprevir). Expression of the HCV NS3 proteases resulted in cleavage of the lambda cI repressor with MAVS cleavage site. Expression of the protease was induced with IPTG for 3 h. The lambda cI repressor with MAVS cleavage site was not cleaved by an NS3 protease that included a substitution in catalytic residue S139A. Similarly, different catalytic efficiencies were observed with different proteases.
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S2851 |
Baricitinib (INCB028050)Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
![]() ![]() bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test. |
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S2485 |
Mitoxantrone 2HClMitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
![]() ![]() Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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S1759 |
Pitavastatin CalciumPitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis. |
![]() ![]() Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
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S1401 |
TenofovirTenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections. |
![]() ![]() The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; **** p<0.0001; *** p<0.001 (unpaired t-test). |
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S2823 |
TideglusibTideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2. |
![]() ![]() (A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs. |
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S3035 |
Daunorubicin HClDaunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
![]() ![]() A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. *p<0.05, **p<0.01, ***p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown). |
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S1386 |
Nafamostat MesylateNafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
![]() ![]() Immunofluorescence of NF-κB/p65 in HCT 116 and SW 1116 cells exposed to TNFα (25 ng/ml) with or without nafamostat mesilate(FLU) (100 μM). Scale bars: 20 μm. |
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S1680 |
DisulfiramDisulfiram (NSC 190940) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. |
![]() ![]() The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “*” for p<0.05 or “**” for p<0.01. |
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S1706 |
LamivudineLamivudine (GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase. |
![]() ![]() The indicated liver cancer cell lines—Hep-3B, Huh-7 and PLC were treated with or without 5 types anti-hepatitis B virus drugs (C) with the concentration of 100 μM, and M1 virus (MOI = 10) for 72 hours. Following 72 hours, cell viabilities were determined by MTT assay (mean ± SD). N.S. Not significant.
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S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
![]() ![]() HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. *P < 0.05, **P < 0.01, ***P < 0.001, 1-way ANOVA with Dunnett’s post-test. |
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S4157 |
Chloroquine diphosphateChloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
![]() ![]() NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
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S1351 |
IvermectinIvermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
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S1289 |
CarmofurCarmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
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S4028 |
Dexamethasone Sodium PhosphateDexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S1835 |
AzithromycinAzithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
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S3037 |
Bepotastine BesilateBepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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S2874 |
Camostat MesilateCamostat (FOY-305) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase. |
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S3124 |
Dexamethasone AcetateDexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S3079 |
AtovaquoneAtovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia. |
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S2079 |
Moexipril HClMoexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure. |
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S1691 |
PraziquantelPraziquantel is an anthelmintic effective against flatworms. |
![]() ![]() Schistosomicidal effects of PZQ, ART and OXA on 14-day-schistosomula. Magnification of the in vitro-cultured schistosomula treated with PZQ, ART, and OXA at 10 μM. Drugs were added at day 14 and schistosomula were analyzed at day 21 (late treatment). 0.1% DMSO in medium (solvent of the drugs; used as negative control) had no effect on schistosomula development. |
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S2926 |
TDZD-8TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. |
![]() ![]() The impact of GSK3β inhibitor TDZD-8 (10 μM) on the GSK3β phosphorylation (A), the protein expression (B) and mRNA level (C) of α-SMA and collagen I in acetaldehyde-induced HSCs activation. The data were representative of at least three independent experiments. All values were expressed as mean ± SD. *P < 0.01, ***P < 0.01 vs. the control group, #P < 0.05, ##P < 0.01, ###P < 0.01 vs. the acetaldehyde group.
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S7393 |
Aloxistatin(E64d)Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. |
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S8279 |
ShikoninShikonin (nchusin, Anchusa acid, Alkanna Red, C.I. 75535, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
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S7975 |
Favipiravir (T-705)Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections. |
![]() ![]() (A) BoDV-1 infection was measured by IFA. BoDV-1 P40 was detected with a primary monoclonal antibody (red), nuclei were stained with DAPI (blue), merged image (scale bars: 50 μm). Favipiravir: T-705
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S5250 |
DarunavirDarunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
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S5940 |
BepotastineBepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
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S5754 |
Baricitinib phosphateBaricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
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S7392 |
Loxistatin Acid (E-64C)Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
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S7262 |
VidofludimusVidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2. |
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S7947 |
PX-12PX-12 is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2. |
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S5911 |
BictegravirBictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase. |
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S4646 |
CiclesonideCiclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases. |
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S4430 |
Hydroxychloroquine SulfateHydroxychloroquine Sulfate (HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9. |
![]() ![]() C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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S7579 |
Ledipasvir (GS5885)Ledipasvir (GS5885) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection. |
![]() ![]() (C) Impact of HCV clearance by DAA treatment on the Nrf2 nuclear translocation. HCV infected Huh-7.5 cells day 12 were given two rounds of antiviral treatment with IFN-α, sofosbuvir, ledipasvir or combination of sofosbuvir plus ledipasvir. After 72 hours, cells were split, and then treated again with the same antiviral agent. After two rounds of antiviral treatment, the expressions of HCV core and pNrf2 were measured by immunostaining.
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S9567 |
Indinavir SulfateIndinavir sulfate is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS. |
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S3724 |
VelpatasvirVelpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
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S3733 |
BoceprevirBoceprevir is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. |
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S2071 |
Prulifloxacin (NM441)Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. |
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S4282 |
Nelfinavir MesylateNelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S2853 |
Carfilzomib (PR-171)Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis. |
![]() ![]() Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,
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S1185 |
RitonavirRitonavir (ABT-538, A 84538) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis. |
![]() ![]() (A) KMS11 and
(B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown).
(C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to
untreated cells (not shown).
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S1538 |
Telaprevir (VX-950)Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM. |
![]() ![]() HCV replicon genotype 1b cells were passaged in the presence of G418 alone (medium 694 control) or G418 with miravirsen, SPC4729 (oligonucleotide negative control) or telaprevir for 28 days in fixed concentrations at a multiple (X) of the EC50 of miravirsen or telaprevir. Colony formation was assessed by staining surviving cells with crystal violet.
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S1380 |
LopinavirLopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
![]() ![]() Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
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S1322 |
DexamethasoneDexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S0833新 |
EIDD-1931EIDD-1931 (NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
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S8969新 |
Molnupiravir (EIDD-2801)Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
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S8932新 |
Remdesivir (GS-5734)Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
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S6676新 |
EbselenEbselen (DR 3305, SPI-1005, PZ-51) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. |
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S2169 |
Rosuvastatin CalciumRosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay. |
![]() ![]() MDA-MB-231 cells were treated with simvastatin (SIM) or rosuvastatin (ROSU) in combination with ZOL for 48 h. Vitality and apoptosis were measured by using the cell titer blue and the caspase 3/7 Glo assay. Data are shown as mean ± SD of at least three individual experiments (*p ≤ 0.05; **p ≤ 0.01; ***p ≤ 0.001). |
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S1183 |
Danoprevir (ITMN-191)Danoprevir (ITMN-191, RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2. |
![]() ![]() Western blot analysis of HCV NS3 protease cleavage of MAVS. The catalytic efficiency of four proteases (H, H-A156T, 41 and 41-A156T) from individuals H and 41 were tested in the absence or presence of an NS3 protease inhibitor (danoprevir). Expression of the HCV NS3 proteases resulted in cleavage of the lambda cI repressor with MAVS cleavage site. Expression of the protease was induced with IPTG for 3 h. The lambda cI repressor with MAVS cleavage site was not cleaved by an NS3 protease that included a substitution in catalytic residue S139A. Similarly, different catalytic efficiencies were observed with different proteases.
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S2851 |
Baricitinib (INCB028050)Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3. |
![]() ![]() bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test. |
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S2485 |
Mitoxantrone 2HClMitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
![]() ![]() Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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S1759 |
Pitavastatin CalciumPitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis. |
![]() ![]() Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
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S1401 |
TenofovirTenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections. |
![]() ![]() The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; **** p<0.0001; *** p<0.001 (unpaired t-test). |
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S2823 |
TideglusibTideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2. |
![]() ![]() (A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs. |
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S3035 |
Daunorubicin HClDaunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
![]() ![]() A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. *p<0.05, **p<0.01, ***p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown). |
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S1386 |
Nafamostat MesylateNafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
![]() ![]() Immunofluorescence of NF-κB/p65 in HCT 116 and SW 1116 cells exposed to TNFα (25 ng/ml) with or without nafamostat mesilate(FLU) (100 μM). Scale bars: 20 μm. |
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S1680 |
DisulfiramDisulfiram (NSC 190940) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. |
![]() ![]() The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “*” for p<0.05 or “**” for p<0.01. |
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S1706 |
LamivudineLamivudine (GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase. |
![]() ![]() The indicated liver cancer cell lines—Hep-3B, Huh-7 and PLC were treated with or without 5 types anti-hepatitis B virus drugs (C) with the concentration of 100 μM, and M1 virus (MOI = 10) for 72 hours. Following 72 hours, cell viabilities were determined by MTT assay (mean ± SD). N.S. Not significant.
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S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
![]() ![]() HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. *P < 0.05, **P < 0.01, ***P < 0.001, 1-way ANOVA with Dunnett’s post-test. |
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S4157 |
Chloroquine diphosphateChloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
![]() ![]() NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
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S1351 |
IvermectinIvermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
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S1289 |
CarmofurCarmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
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S4028 |
Dexamethasone Sodium PhosphateDexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S1835 |
AzithromycinAzithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
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S3037 |
Bepotastine BesilateBepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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S2874 |
Camostat MesilateCamostat (FOY-305) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase. |
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S3124 |
Dexamethasone AcetateDexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S3079 |
AtovaquoneAtovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia. |
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S2079 |
Moexipril HClMoexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure. |
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S1691 |
PraziquantelPraziquantel is an anthelmintic effective against flatworms. |
![]() ![]() Schistosomicidal effects of PZQ, ART and OXA on 14-day-schistosomula. Magnification of the in vitro-cultured schistosomula treated with PZQ, ART, and OXA at 10 μM. Drugs were added at day 14 and schistosomula were analyzed at day 21 (late treatment). 0.1% DMSO in medium (solvent of the drugs; used as negative control) had no effect on schistosomula development. |
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S2926 |
TDZD-8TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. |
![]() ![]() The impact of GSK3β inhibitor TDZD-8 (10 μM) on the GSK3β phosphorylation (A), the protein expression (B) and mRNA level (C) of α-SMA and collagen I in acetaldehyde-induced HSCs activation. The data were representative of at least three independent experiments. All values were expressed as mean ± SD. *P < 0.01, ***P < 0.01 vs. the control group, #P < 0.05, ##P < 0.01, ###P < 0.01 vs. the acetaldehyde group.
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S7393 |
Aloxistatin(E64d)Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. |
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S8279 |
ShikoninShikonin (nchusin, Anchusa acid, Alkanna Red, C.I. 75535, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
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S7975 |
Favipiravir (T-705)Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections. |
![]() ![]() (A) BoDV-1 infection was measured by IFA. BoDV-1 P40 was detected with a primary monoclonal antibody (red), nuclei were stained with DAPI (blue), merged image (scale bars: 50 μm). Favipiravir: T-705
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S5250 |
DarunavirDarunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
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S5940 |
BepotastineBepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
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S5754 |
Baricitinib phosphateBaricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
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S7392 |
Loxistatin Acid (E-64C)Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry. |
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S7262 |
VidofludimusVidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2. |
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S7947 |
PX-12PX-12 is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2. |
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S5911 |
BictegravirBictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase. |
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S4646 |
CiclesonideCiclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases. |
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S4430 |
Hydroxychloroquine SulfateHydroxychloroquine Sulfate (HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9. |
![]() ![]() C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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S7579 |
Ledipasvir (GS5885)Ledipasvir (GS5885) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection. |
![]() ![]() (C) Impact of HCV clearance by DAA treatment on the Nrf2 nuclear translocation. HCV infected Huh-7.5 cells day 12 were given two rounds of antiviral treatment with IFN-α, sofosbuvir, ledipasvir or combination of sofosbuvir plus ledipasvir. After 72 hours, cells were split, and then treated again with the same antiviral agent. After two rounds of antiviral treatment, the expressions of HCV core and pNrf2 were measured by immunostaining.
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S9567 |
Indinavir SulfateIndinavir sulfate is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS. |
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S3724 |
VelpatasvirVelpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. |
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S3733 |
BoceprevirBoceprevir is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. |
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S2071 |
Prulifloxacin (NM441)Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. |
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S4282 |
Nelfinavir MesylateNelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM. |