新製品

添加時期順序で新製品が表示されます。

PI3K/Akt/mTOR
製品コード 製品名称 製品説明 添加時期
S6811 Miransertib (ARQ-092) Miransertib (ARQ-092) is a potent, selective and orally bioavailable allosteric inhibitor of Akt with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Jul 13 2020
S0177 XMD-17-51 XMD-17-51 is a potent and highly selective inhibitor of NUAK1. Jul 06 2020
S8953 ASP4132 ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer. Jul 01 2020
S2272 Indoprofen Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. Apr 02 2020
S8500 BAY1125976 BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP). Mar 25 2020
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. Feb 26 2020
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis. Feb 26 2020
S8581 Serabelisib (TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. Feb 26 2020
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2. Feb 26 2020
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Phase 2. Feb 26 2020
JAK/STAT
製品コード 製品名称 製品説明 添加時期
S0391 TG-89 TG-89 is a JAK inhibitor that inhibits JAK2, FLT3, RET and JAK3. May 26 2020
S1050 TCS PIM-1 1 TCS PIM-1 1 is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM. May 07 2020
S6784 STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. Apr 15 2020
S6774 TP-3654 TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively. Apr 08 2020
S7985 PIM447 (LGH447) PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis. Mar 10 2020
S7650 Peficitinib (ASP015K) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3. Feb 26 2020
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. Feb 25 2020
S2789 Tofacitinib (CP-690550) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis. Feb 25 2020
S2736 Fedratinib (TG101348) Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and Ret with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. Feb 25 2020
S7634 Cerdulatinib (PRT062070) Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. Feb 25 2020
Cell Cycle
製品コード 製品名称 製品説明 添加時期
S8906 MYCi975 MYCi975 is an orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities. Jul 14 2020
S8916 BI-3406 BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities. Jul 14 2020
S8905 MYCi361 MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. Jul 08 2020
S8730 BAY 1251152 BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. Jul 06 2020
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC) Jun 29 2020
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis. Jun 08 2020
S0500 Purvalanol B Purvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. May 26 2020
S7969 THZ2 Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity. May 26 2020
S6836 TH-257 TH-257 is a potent and exquisitely selective LIM kinase (LIMK) inhibitor with IC50 of 84 nM and 39 nM for LIMK1 and LIMK2, respectively. May 26 2020
S8903 AS2863619 AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells. May 26 2020
DNA Damage
製品コード 製品名称 製品説明 添加時期
S0054 D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively. Jul 14 2020
S6854 Triazavirin Triazavirin is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza. Jul 14 2020
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells. Jul 06 2020
S0102 L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage. Jun 15 2020
S0469 ML216 ML216 is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively. May 26 2020
S8876 RK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. May 19 2020
S8962 BRD3308 BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. May 14 2020
S2600 Fexinidazole Fexinidazole is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness). Apr 02 2020
S1764 Rifampin Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections. Mar 08 2020
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. Feb 26 2020
TGF-beta/Smad
製品コード 製品名称 製品説明 添加時期
S0523 SB 4 (Eticovo) SB 4 (Eticovo) is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 (Eticovo) enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. Jun 02 2020
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34 nM. Mar 08 2020
A2113 Anti-human/mouse TGF-β-InVivo The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody. Mar 06 2020
S7530 Vactosertib Vactosertib  (TEW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. Feb 26 2020
S7208 Bisindolylmaleimide I (GF109203X) Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. Feb 24 2020
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 09 2020
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Dec 19 2019
S6713 ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. Nov 07 2019
S7663 LY333531 HCl LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. Aug 05 2019
S1292 Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 mM. Jul 21 2019
GPCR & G Protein
製品コード 製品名称 製品説明 添加時期
S0555 Adomeglivant Adomeglivant is a potent and selective antagonist of glucagon receptor that is used as a chronic treatment for type 2 diabetes. Jul 06 2020
S9608 AB928 AB928 is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively. Jun 30 2020
S8017 WIN 55, 212-2 mesylate WIN 55,212-2 Mesylate is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. Jun 29 2020
S0295 Anavex 2-73 HCl Anavex 2-73, an aminotetrahydrofuran derivative, is a mixed muscarinic and sigma-1/σ1 Receptor agonist with IC50 of 0.86 μM. Jun 02 2020
S6806 SBI-115 SBI-115 is a novel TGR5 (GPCR19) antagonist. SBI-115 decreases cell proliferation, cholangiocyte spheroid growth and cAMP levels in cystic cholangiocytes. May 26 2020
S6793 TG4-155 TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. Apr 08 2020
S6621 CCG215022 CCG215022 serves as a pan-G protein-coupled receptor kinases (GRKs) inhibitor with IC50 of 3.9 μM, 0.15 μM, 0.38 μM for GRK1, GRK2, GRK5, respectively. Mar 11 2020
S6659 Rimegepant (BMS-927711) Rimegepant is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM. Feb 26 2020
S1151 Ibutamoren mesylate A potent, orally active growth hormone (GH) secretagogue. Feb 26 2020
S5753 Setipiprant(ACT-129968) Setipiprant(ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1. Feb 25 2020
Protein Tyrosine Kinase
製品コード 製品名称 製品説明 添加時期
S8852 Pyrotinib (SHR-1258) Pyrotinib (SHR-1258) is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively. Jun 08 2020
S7688 Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. Jun 03 2020
S6805 Tyrphostin AG-528 Tyrphostin AG-528 is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity. Jun 03 2020
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions of Acetylcysteine are best fresh-prepared. Jun 03 2020
S6843 X-82 (Vorolanib) Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. Jun 03 2020
S8879 BMS-986165 BMS-986165 is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. Jun 02 2020
S0487 Sulfatinib Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. Jun 02 2020
S0360 EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics. May 19 2020
S8933 ONO-7475 ONO-7475 is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells. May 07 2020
S6813 Mobocertinib (TAK788) Mobocertinib (TAK788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent. Apr 28 2020
Epigenetics
製品コード 製品名称 製品説明 添加時期
S0201 Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. Jul 06 2020
S8889 MZ-1 MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. Jul 01 2020
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling. Jun 03 2020
S0269 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members. May 19 2020
S8812 CM272 CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death. Mar 25 2020
S6687 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. Mar 25 2020
S6548 NKL 22 NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. Mar 17 2020
S1073 BML-210 (CAY10433) BML-210 is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. Mar 17 2020
S6738 TC-H 106 TC-H 106 is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. Mar 17 2020
S2132 SR-4370 SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. Mar 17 2020
NF-κB
製品コード 製品名称 製品説明 添加時期
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε. Jul 06 2020
S8922 TBK1/IKKε-IN-1(compound 1) TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. May 14 2020
S6671 SN50 SN50, a cell-permeable NF-κB inhibitory peptide, is composed of the signal peptide of Kaposi fibroblast growth factor.SN50 inhibits the activation of NF-κB and attenuates ventilator-induced lung injury. Mar 25 2020
S8044 BMS-345541 BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. Nov 17 2019
S6714 INH14 INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively. Nov 07 2019
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases. Aug 13 2019
S7352 Bay 11-7085 BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. May 07 2019
S2864 IMD 0354 IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. Feb 21 2019
S4902 QNZ (EVP4593) QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively. Feb 21 2019
S2913 BAY 11-7082 BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. Also inhibiting components of the ubiquitin system. Nov 28 2018
Metabolism
製品コード 製品名称 製品説明 添加時期
S8997 680C91 680C91 is a potent and selective inhibitor of TDO with Ki of 51 nM. Jul 14 2020
S0718 AG-120 (racemic) AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. Jul 06 2020
S0018 Verdiperstat Verdiperstat (AZD3241) is a selective, orally active and irreversible inhibitor of myeloperoxidase (MPO) with IC50 of 630 nM. Verdiperstat (AZD3241) can be used in the research of neurodegenerative brain disorders. Jul 06 2020
S0277 BMS303141 BMS-303141 is a potent, cell-permeable inhibitor of ATP-citrate lyase (ACL) with IC50 of 0.13 μM. BMS-303141 shows inhibition of total lipid syntheses with IC50 of 8 μM in HepG2 cells. Jul 06 2020
S7321 FIPI FIPI, a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively. Jul 06 2020
S0788 ML210 ML-210 is a selective covalent inhibitor of cellular glutathione peroxidase 4 (GPX4) with EC50 of 0.04 μM and induces ferroptosis. ML-210 can selectively kill cells induced to express mutant RAS. ML-210 exhibits anti-cancer activity. Jun 29 2020
S0136 KY-226 KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. Jun 29 2020
S8980 SBI-797812 SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. SBI-797812 turns NAMPT into a "super catalyst" that more efficiently generates NMN. Jun 24 2020
S8995 BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors. Jun 24 2020
S0118 SBC-110736 SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9) that lowers cholesterol levels in mice. Jun 23 2020
Proteases
製品コード 製品名称 製品説明 添加時期
S0475 GC376 sodium GC376 is a 3CLpro (3C-like protease) inhibitor with IC50 of ~ 1.11 μM for the PEDV 3CLpro. GC376 is active against the 3CLpro of multiple coronaviruses, including SARS-CoV. Jul 14 2020
S0769 MMP-9-IN-1 MMP-9-IN-1 is a specific inhibitor of matrix metalloproteinase-9 (MMP-9). MMP-9-IN-1 selectively targets the hemopexin (PEX) domain of MMP-9 with Kd of 2.1 μM. Jun 29 2020
S6830 o-Phenanthroline o-Phenanthroline, a hypoxia-mimicking agent, is a non-specific matrix metalloproteinase (MMP) inhibitor with IC50 of 110.5μM for Collagenase. O-phenanthroline reduces the expression of MMP3 and MMP13 mRNA levels during chondrogenic differentiation of human chondrocytes (hChs), as well as after TNFα/IL-1β exposure in an explant model. o-Phenanthroline is also a metal chelator which prevents the induction of chromosomal aberrations in streptozotocin-treated cells and forms a red chelate with Fe2+ that absorbs maximally at 510 nm. Apr 28 2020
S4163 Doxycycline Hyclate Doxycycline is a member of the tetracycline antibiotics group, and is commonly used to treat a variety of infections. It is also an inhibitor of matrix metallo-proteinases (MMP). Mar 13 2020
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2. Feb 26 2020
S8455 Talabostat (PT-100) Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. Feb 25 2020
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007) is a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase, targeting NS5B polymerase. Feb 25 2020
S8891 JHU-083 JHU-083 is a novel prodrug of DON.JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress. Solutions are best fresh-prepared. Feb 14 2020
S1575 RO4929097 RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2. Jan 19 2020
S2619 MG-132 MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells. Jan 07 2020
Microbiology
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S6848 3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer. Jun 22 2020
S4307 Auranofin Auranofin (SKF-39162) is an inhibitor of thioredoxin reductase (TrxR) with IC50 of 88 nM for purified H. pylori TrxR in cell-free assay. Auranofin has anti-cancer activity and can completely inhibit bacterial growth at 1.2 μM. Auranofin is an FDA-approved gold-containing compound used for the treatment of rheumatoid arthritis. Jun 08 2020
S6771 MAC-545496 MAC-545496 is a nanomolar glycopeptide-resistance-associated protein R(GraR) inhibitor with strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 can reverse β-lactam resistance in methicillin-resistant strains and synergize with CAMPs. MAC-545496 shows remarkable activity in macrophages and attenuates S. aureus virulence in a G. mellonella larvae infection model. Jun 08 2020
S0443 Desciclovir Desciclovir (DCV) is a prodrug of the antiherpetic agent acyclovir (ACV) that converted into ACV by xanthine oxidase in humans. Jun 08 2020
S0436 Pleconaril Pleconaril is a capsid inhibitor used previously to treat enterovirus infections. Pleconaril is effective in inhibiting replication with IC50 of < 0.050 μM. May 26 2020
S0470 RSV604 RSV604, a novel benzodiazepine, is an inhibitor of respiratory syncytial virus (RSV) with EC50 of 0.86 μM. RSV604 has significant potential for the effective treatment of RSV disease. Phase 2. May 26 2020
S4408 Procodazole Procodazole is used as a potentiator which is non-specific active immunoprotective against viral and bacterial infections. May 25 2020
S8969 EIDD-2801 EIDD-2801 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. May 20 2020
S0285 Bay 41-4109 racemate BAY 41-4109 racemate is a mixture of R-isomer of BAY 41-4109 and S-isomer of BAY 41-4109. BAY 41-4109 an antiviral compound that inhibits human hepatitis B virus (HBV) with IC50 of 53 nM. May 19 2020
S0038 AB-423 AB-423, a member of the sulfamoylbenzamide (SBA) class of hepatitis B virus (HBV) capsid inhibitors, shows potent inhibition of HBV replication with EC50 of 0.08 μM - 0.27 μM and EC90 of 0.33 μM - 1.32 μM in cells. Phase 1. May 19 2020
Apoptosis
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S8845 GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities. Jul 08 2020
S0096 S-Gboxin S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM. Jun 02 2020
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. May 26 2020
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate, also known as Teroxirone, is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry. Apr 15 2020
S2465 CPI-1189 CPI-1189 is the proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor. CPI-1189 intracellularly inhibits the p38 mitogen-activated protein kinase phosphoactivation and shows neuroprotective effects. Apr 02 2020
S6679 C25-140 C25-140 is a small-molecule inhibitor of TRAF6-Ubc13 interaction. C25-140 directly binds to TRAF6, thereby blocking the interaction of TRAF6 with Ubc13, and as a consequence lowers TRAF6 activity. C25-140 impedes NF-κB activation in various immune and inflammatory signaling pathways also in primary human and murine cells. Mar 25 2020
S8927 GSK2983559 (compound 3) GSK2983559 is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity. Mar 25 2020
S8250 79-6 (CID5721353) 79-6 (CID5721353) is a BCL6 inhibitor with Kd value of 138 μM. Feb 26 2020
S8759 S55746 S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds. Feb 26 2020
S8781 Selpercatinib (LOXO-292) Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively. Feb 26 2020
MAPK
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S7794 JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. Jul 01 2020
S8900 SR18662 SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis. Jul 01 2020
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71. Apr 15 2020
S6786 ERK5-IN-2 ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50 of 0.82 μM and 3 μM for ERK5 and ERK5 MEF2D, respectively. Apr 15 2020
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. Apr 08 2020
S6680 L-779450 L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM. Mar 17 2020
S8125 Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms. Feb 26 2020
S1089 Refametinib (RDEA119) Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. Feb 26 2020
S7854 Ulixertinib (BVD-523) Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1. Feb 26 2020
S8853 Belvarafenib Belvarafenib (GDC5573, HM95573, RG6185) is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. Feb 26 2020
Angiogenesis
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S0020 RK 24466 RK-24466 (KIN 001-51) is a potent and selective inhibitor of Lck that inhibits two constructs of the human lck kinase, lck (64-509) and lckcd with IC50 of < 0.001 μM and 0.002 μM, respectively. Jul 14 2020
S0088 Pemigatinib (INCB054828) Pemigatinib (INCB054828) is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma. Jul 06 2020
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide. Apr 28 2020
S8888 GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. Apr 22 2020
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. Apr 08 2020
S6684 IOX4 IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. Apr 02 2020
S2213 AMG-47a AMG-47a is a potent, nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation. AMG-47a exhibit anti-inflammatory activity (ED50) of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2) in mice. Apr 02 2020
S1099 SKLB4771 (FLT3-IN-1) SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10 nM. Mar 17 2020
S7028 Duvelisib (IPI-145) Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. Feb 26 2020
S2183 BGJ398 (NVP-BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2. Feb 26 2020
Stem Cells & Wnt
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S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. Jul 14 2020
S8951 TED-347 TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. Jun 03 2020
S2249 PF 4800567 PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM). Mar 08 2020
S2151 Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3. Feb 26 2020
S1146 Cyclopamine Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. Dec 19 2019
S6745 JW55 JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). Dec 05 2019
S7143 LGK974 LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1. Nov 26 2019
S6616 ETC-159 ETC-159 is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells. Nov 04 2019
S1082 Vismodegib (GDC-0449) Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay. Sep 20 2019
S5815 WAY-316606 WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb. Aug 26 2019
Neuronal Signaling
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S0398 Astemizole Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects. Jul 14 2020
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptor (DRD2) and has broad-spectrum anti-tumor activity. Jul 14 2020
S0313 Volinanserin Volinanserin is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. Jun 02 2020
S0779 Pirenperone Pirenperone, a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). Jun 02 2020
S4389 Bephenium Hydroxynaphthoate Bephenium is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis. May 25 2020
S0222 Lvguidingan Lvguidingan (Anticonvulsant 7903) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. May 19 2020
S2649 SB 200646 SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. May 07 2020
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator. Apr 22 2020
S6787 KN-93 KN-93 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity. Apr 22 2020
S2646 VU0238429 VU0238429 is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4. Apr 22 2020
その他
製品コード 製品名称 製品説明 添加時期
S0279 Dimethylenastron Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells. Jul 14 2020
S0054 D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively. Jul 14 2020
S8837 FB23-2 FB23-2 is a potent and selective FTO inhibitor that directly binds to FTO and selectively inhibits FTO's N6-methyladenosine (m6A) demethylase activity with IC50 of 2.6 μM. Jul 14 2020
S6834 CM 4620 CM 4620 is an inhibitor of calcium-release activated calcium-channel (CRAC channel). CM4620 inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of near 120 nM and 900 nM, respectively. Jul 14 2020
S6854 Triazavirin Triazavirin is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza. Jul 14 2020
S8976 DCLK1-IN-1 DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively. Jul 14 2020
S0308 AMZ30 AMZ30 is a selective and covalent inhibitor of protein phosphatase methylesterase-1(PME-1) with IC50 of 0.60 μM. AMZ30 reduces the demethylated form of PP2A in living cells. Jul 06 2020
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells. Jul 06 2020
S0338 NB 598 NB-598 is a potent, competitive squalene epoxidase (SE) inhibitor. NB-598 suppresses cholesterol biosynthesis. Jul 06 2020
S0485 Hoechst 33342 Hoechst 33342 is a membrane-permeant fluorescent stain that can stain live cells. Hoechst 33342 binds to adenine-thymine-rich regions of DNA in the minor groove. Jul 06 2020