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
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2. Apr 20 2018
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1. Apr 20 2018
S1120 Everolimus (RAD001) Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Apr 20 2018
S2814 Alpelisib (BYL719) Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2. Apr 20 2018
S2247 Buparlisib (BKM120, NVP-BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2. Apr 20 2018
S7840 Dorsomorphin (Compound C, BML-275) Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity. Apr 20 2018
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. Apr 15 2018
S7335 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. Apr 03 2018
S8194 TGR-1202 TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. Mar 29 2018
S7937 GSK2269557 Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). Mar 29 2018
JAK/STAT
製品コード 製品名称 製品説明 添加時期
S7024 Stattic Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Apr 20 2018
S8195 Oclacitinib maleate Oclacitinib(PF 03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. Apr 15 2018
S8605 C188-9 C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. Apr 13 2018
S8538 PF-06651600 PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. Apr 03 2018
S7951 STA-21 Ochromycinone (STA-21) is a selective STAT3 inhibitor. Feb 10 2018
S8541 FM-381 FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. Jan 24 2018
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Jan 16 2018
A5084 STAT6 Rabbit Recombinant mAb   Jan 16 2018
A5159 JAK1 Rabbit Recombinant mAb WBELISA Jan 12 2018
S2902 S-Ruxolitinib (INCB018424) S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. Oct 27 2017
Cell Cycle
製品コード 製品名称 製品説明 添加時期
S8699 SNS-314   Apr 20 2018
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Phase 3. Apr 20 2018
S7440 Ribociclib (LEE011) Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3. Apr 20 2018
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3. Apr 20 2018
S8652 Skp2 inhibitor C1 (SKPin C1)   Apr 19 2018
S8208 Hydroxyfasudil (HA-1100) HCl Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively. Apr 15 2018
S8156 ARS-853 (ARS853) ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. Apr 15 2018
S1525 Adavosertib (MK-1775) MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2. Mar 29 2018
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. Mar 12 2018
S7687 GSK269962 HCl GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. Feb 25 2018
DNA Damage
製品コード 製品名称 製品説明 添加時期
S1060 Olaparib (AZD2281, Ku-0059436) 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. Apr 20 2018
S7048 Talazoparib (BMN 673) Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. Apr 20 2018
S1782 Azacitidine Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Apr 20 2018
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells. Apr 20 2018
S8419 E7449 E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. Apr 15 2018
S5111 7-Ethylcamptothecin 7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. Apr 03 2018
S4782 5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. Apr 03 2018
A5389 Thymidine Kinase 1 Rabbit Recombinant mAb WB,ELISA Apr 02 2018
S3898 Hydroxy Camptothecine 10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. Mar 15 2018
S8666 BAY 1895344 (BAY-1895344) BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. Jan 24 2018
TGF-beta/Smad
製品コード 製品名称 製品説明 添加時期
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. Mar 29 2018
S7207 Bisindolylmaleimide IX (Ro 31-8220 Mesylate) Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1. Feb 10 2018
S7530 Vactosertib  (TEW-7197) 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 10 2018
A5114 Bim Rabbit Recombinant mAb WBELISA Jan 12 2018
A5117 Smad2 Rabbit Recombinant mAb WBELISA Jan 12 2018
A5130 Smad4 Rabbit Recombinant mAb WBELISA Jan 12 2018
A5135 PKC delta Rabbit Recombinant mAb WBELISA Jan 12 2018
A5155 PKC epsilon Rabbit Recombinant mAb WBELISA Jan 12 2018
A5162 PKC alpha Rabbit Recombinant mAb WBELISA Jan 12 2018
A5192 Phospho-Smad2 (S250) Rabbit Recombinant mAb WBELISA Jan 12 2018
GPCR & G Protein
製品コード 製品名称 製品説明 添加時期
S4932 Proxyphylline   Apr 19 2018
S3988 Theophylline-7-acetic acid Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. Apr 17 2018
A5426 DARPP32 Rabbit Recombinant mAb   Mar 29 2018
S7174 Opaganib (ABC294640) Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2. Feb 10 2018
S3734 Albiglutide Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist). Jan 23 2018
A5270 GRK2 Rabbit Recombinant mAb   Jan 17 2018
S7177 PF-543 PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. Jan 16 2018
A5415 ADORA1 Rabbit Recombinant mAb   Jan 09 2018
S1647 Adenosine Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. Jan 08 2018
S3051 Bosentan Hydrate Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. Dec 05 2017
Protein Tyrosine Kinase
製品コード 製品名称 製品説明 添加時期
S7297 AZD9291 Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. Apr 20 2018
S1023 Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Apr 20 2018
S1056 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1. Apr 20 2018
S2841 R428 (BGB324) R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). Apr 20 2018
S2897 ZM 306416 ZM 306416 is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM. Apr 03 2018
S8675 H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively). Mar 07 2018
S7674 HMPL-504(AZD6094, Volitinib) Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. Mar 06 2018
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. Feb 28 2018
S3759 Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. Feb 11 2018
S1361 Glesatinib (MGCD265) Glesatinib (MGCD265) is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. Feb 10 2018
Epigenetics
製品コード 製品名称 製品説明 添加時期
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor. Apr 13 2018
S8664 GSK3326595 (EPZ015938) GSK3326595 (EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. Apr 13 2018
S7230 UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. Apr 03 2018
S8479 LLY-283 LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. Apr 03 2018
S8627 OSS_128167 OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. Mar 02 2018
S8495 WT161 WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. Mar 02 2018
S8071 UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. Feb 08 2018
S7574 GSK-LSD1 2HCl GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). Feb 02 2018
S3944 Valproic acid Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers. Jan 25 2018
S1047 Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Jan 24 2018
NF-κB
製品コード 製品名称 製品説明 添加時期
S3633 Pyrrolidinedithiocarbamate ammonium Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines. Apr 13 2018
A5168 p120 (Catenin Delta 1) Rabbit Recombinant mAb WBELISA Jan 12 2018
A5395 RelB Rabbit Recombinant mAb   Jan 09 2018
A5071 IKK beta Rabbit Recombinant mAb   Nov 08 2017
A5075 NF-kB p65 Rabbit Recombinant mAb   Nov 08 2017
S8261 GSK583 GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. Feb 09 2017
S4712 Diethylmaleate Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB. Oct 26 2016
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. Apr 25 2016
S7691 PS-1145 PS-1145 is a specific IKK inhibitor with IC50 of 88 nM. Mar 09 2016
S7851 AZD3264 AZD3264 is a novel IKK2 inhibitor. Nov 27 2015
Metabolism
製品コード 製品名称 製品説明 添加時期
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Apr 20 2018
S4837 Ibudilast   Apr 19 2018
S4856 Iproniazid   Apr 19 2018
S5014 Crisaborole (AN2728)   Apr 19 2018
S4930 Cetilistat Cetilistat is a novel highly lipophilic benzoxazinone that inhibits gastrointestinal and pancreatic lipases. It shows a good safety and tolerability profile in vivo Apr 17 2018
S8244 Etomoxir (Na salt) Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Apr 16 2018
S8254 FIN56 FIN56 is a specific inducer of ferroptosis . Apr 12 2018
S4063 Vitamin D3 Vitamin D3 is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM. Mar 29 2018
S2687 PF-2545920 PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. Mar 29 2018
S8557 IDO inhibitor 1 IDO inhibitor 1 is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) with IC50 of 3 nM. Mar 22 2018
Proteases
製品コード 製品名称 製品説明 添加時期
S4935 Asunaprevir Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication. Apr 17 2018
S5015 Simeprevir Simeprevir is a competitive, reversible, macrocyclic, noncovalent hepatitis C virus (HCV) NS3/4A protease inhibitor that acts directly against the hepatitis C virus. It has a medium inhibitory concentration (IC50) <13 nM for all HCV NS3/4A enzymes(genotypes 1a, 1b, 2, 4, 5, and 6), but has an IC50 value of 37 nM for genotype 3. Apr 17 2018
S3733 Boceprevir Boceprevir 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. Jan 23 2018
A5284 Cathepsin L/V/K/H Rabbit Recombinant mAb   Jan 18 2018
A5287 Cathepsin B Rabbit Recombinant mAb   Jan 18 2018
A5125 Glutaminase Rabbit Recombinant mAb WBELISA Jan 12 2018
A5396 PAI1 Rabbit Recombinant mAb   Jan 12 2018
A5176 Notch1 Rabbit Recombinant mAb WBELISA Jan 12 2018
S3728 Grazoprevir Grazoprevir anhydrous is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively. Dec 06 2017
S3724 Velpatasvir Velpatasvir is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication. Dec 06 2017
Microbiology
製品コード 製品名称 製品説明 添加時期
S4848 Dalbavancin   Apr 19 2018
S5012 Octenidine Dihydrochloride   Apr 19 2018
S3999 α-santonin α-santonin, a naturally occurring sesquiterpene lactone, is a potent antiparasitic agent. Apr 17 2018
S4812 Ceftizoxime Ceftizoxime is a semisynthetic cephalosporin antibiotic which can be administered intravenously or by suppository. It is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative organisms. Apr 17 2018
S4854 Bedaquiline fumarate Bedaquiline fumarate, an oral diarylquinoline, is a bactericidal antimycobacterial drug. It is a proton-translocating ATP synthetase inhibitor. Apr 17 2018
S4759 p-Coumaric Acid p-Coumaric acid is a hydroxy derivative of cinnamic acid found in a variety of edible plants and is reported to have antioxidant, anti-inflammatory, and antimicrobial activity. Apr 12 2018
S5159 Doxycycline Doxycycline is an antibiotic that is used in the treatment of a number of types of infections caused by bacteria and protozoa. Apr 04 2018
S5164 Chlorotetracycline Chlortetracycline is a tetracycline antibiotic and commonly used to treat conjunctivitis in cats. Apr 04 2018
S4844 Cefcapene Pivoxil Hydrochloride Cefcapene Pivoxil is the pivalate ester prodrug form of cefcapene, a semi-synthetic third-generation cephalosporin with antibacterial activity. Apr 04 2018
S5009 Brivudine Brivudine is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. It is incorporated into the viral DNA and blocks the action of DNA polymerases, thus inhibiting viral replication. Apr 04 2018
Apoptosis
製品コード 製品名称 製品説明 添加時期
S8606 HDM201   Apr 19 2018
S8304 Azoramide Azoramide is a small-molecule modulator of the unfolded protein response (UPR). It improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress. Apr 15 2018
A5432 ASK1 Rabbit Recombinant mAb   Mar 29 2018
S8650 BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells. Mar 02 2018
S7609 GW4869 GW4869 is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM. Feb 02 2018
S8580 COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity. Jan 24 2018
S8483 CBL0137 (CBL-0137) CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex). Jan 24 2018
A5259 APAF1 Rabbit Recombinant mAb   Jan 18 2018
A5272 p73 Rabbit Recombinant mAb   Jan 18 2018
A5273 STK3 Rabbit Recombinant mAb   Jan 18 2018
MAPK
製品コード 製品名称 製品説明 添加時期
S7101 SCH772984 SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells. Apr 20 2018
S1036 PD0325901 PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2. Apr 20 2018
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. Apr 20 2018
S1177 PD98059 PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. Apr 20 2018
S7752 SC1 Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal. Mar 29 2018
S1494 Ralimetinib (LY2228820) Ralimetinib (LY2228820) is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2. Feb 10 2018
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3. Jan 16 2018
A5124 MEKK2 Rabbit Recombinant mAb WBELISA Jan 12 2018
A5165 MEK3 Rabbit Recombinant mAb WBELISA Jan 12 2018
A5191 Phospho-MEK1 (S298) Rabbit Recombinant mAb WBELISA Jan 12 2018
Angiogenesis
製品コード 製品名称 製品説明 添加時期
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Apr 20 2018
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Apr 20 2018
S1526 Quizartinib (AC220) Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 3. Apr 20 2018
S2183 BGJ398 (NVP-BGJ398) BGJ398 (NVP-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. Apr 20 2018
S7257 CNX-774 CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. Apr 20 2018
S2801 AZD4547 AZD4547 is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3. Apr 20 2018
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. Apr 20 2018
A5443 WB,ELISA Apr 16 2018
S8312 NSC228155 NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation. Apr 15 2018
S1369 Bafetinib (INNO-406) Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2. Feb 25 2018
Stem Cells & Wnt
製品コード 製品名称 製品説明 添加時期
S1180 XAV939 XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. Apr 20 2018
S4747 Jervine Jervine is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. Apr 15 2018
S8164 YAP-TEAD Inhibitor 1 (Peptide 17) Peptide 17 is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM. Apr 15 2018
S8320 SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction. Apr 15 2018
S8661 CA3 CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. Mar 16 2018
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. Mar 09 2018
S7169 Crenigacestat (LY3039478) Crenigacestat (LY3039478) is an oral Notch inhibitor with an IC50 of 0.41 nM. Feb 10 2018
S8129 Salinomycin (from Streptomyces albus) Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects. Feb 02 2018
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants. Jan 24 2018
S8647 iCRT3 iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays. Jan 24 2018
Neuronal Signaling
製品コード 製品名称 製品説明 添加時期
S1415 Clopidogrel Clopidogrel is an oral, thienopyridine class antiplatelet agent. Apr 20 2018
S4817 Atenolol Atenolol is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors. Apr 17 2018
S4838 Acotiamide hydrochloride Acotiamide Hydrochloride is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor. Apr 17 2018
S3737 Cangrelor Tetrasodium Cangrelor is a potent, competitive P2Y12 receptor inhibitor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation. Apr 13 2018
S4501 Naloxone HCl Dihydrate Naloxone HCl Dihydrate is an opioid inverse agonist drug used to counter the effects of opiate overdose. Apr 03 2018
S8603 NGP 555 NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically. Apr 03 2018
S6001 LY404039 LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3. Mar 29 2018
A5425 BCHE Rabbit Recombinant mAb   Mar 26 2018
S5131 Homotaurine Homotaurine is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy. Mar 22 2018
S2857 MK-801 (Dizocilpine) (-)-MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. Mar 15 2018
その他
製品コード 製品名称 製品説明 添加時期
S1060 Olaparib (AZD2281, Ku-0059436) 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. Apr 20 2018
S7048 Talazoparib (BMN 673) Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. Apr 20 2018
S2446 Levosimendan Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure. Apr 20 2018
S7252 KPT-330 Selinexor (KPT-330) is an orally bioavailable selective CRM1 inhibitor. Phase 2. Apr 20 2018
S1782 Azacitidine Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Apr 20 2018
S1191 Fulvestrant Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Apr 20 2018
S8047 Dynasore Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Apr 20 2018
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells. Apr 20 2018
S4836 Nilutamide   Apr 19 2018
S4851 Tafluprost   Apr 19 2018