New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
S8839 Borussertib Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt. Dec 11 2019
S6571 BQR695 BQR695 is a quinoxaline that displays sub-micromolar potency against human PI4KIIIβ (IC50~90 nM). Aug 28 2019
S6574 KDU691 KDU691 is a Plasmodium PI4K-specific inhibitor with IC50 values of 0.18 μM and 0.061 μM against hypnozoite forms and liver schizontsm, respectively. Aug 28 2019
S6504 BX517 BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). Jul 31 2019
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. Jul 24 2019
S8693 Selective PI3Kδ Inhibitor 1 (compound 7n) Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. Jun 24 2019
S6414 Apilimod Apilimod is a cell permeable small molecule that specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay. It is also an inhibitor of IL-12/23 and shows no activity toward other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms. Apr 30 2019
S5818 acalisib (GS-9820) acalisib (GS-9820) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. Feb 20 2019
S8803 MK-3903 MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. Feb 14 2019
S8654 ex229 (compound 991) EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK. Jan 09 2019
JAK/STAT
Catalog No. Product Name Information Added
S8162 Upadacitinib (ABT-494) Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1. Aug 21 2019
S6524 NSC 42834 NSC42834 is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM. Jul 31 2019
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM. Jul 24 2019
S8684 Selective JAK3 inhibitor 1 Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK. Jun 11 2019
S8804 PF-06700841 PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. May 08 2019
S8765 PF-04965842 PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. Mar 06 2019
S5917 Solcitinib Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively. Jan 23 2019
S5903 JANEX-1 JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM). Jan 16 2019
S5902 1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range. Jan 16 2019
S5904 WHI-P97 WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays. Jan 09 2019
Cell Cycle
Catalog No. Product Name Information Added
S6636 Azaindole 1 (TC-S 7001) Azaindole 1 (TC-S 7001) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner. Dec 31 2019
S8820 PTC596 PTC596 is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. It inhibits cell proliferation and induces apoptosis in a dose- and time-dependent manner. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines. Dec 09 2019
S6752 Y16 Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). Dec 09 2019
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. Nov 11 2019
S8863 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13. Nov 11 2019
S6727 AX-024 HCl AX-024 blocks the interaction of the CD3ε PRS with SH3.1(Nck). Nov 06 2019
S6710 SGC-GAK-1 SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase. Nov 06 2019
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively. Nov 06 2019
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). Oct 10 2019
S6531 Bohemine Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Sep 11 2019
DNA Damage
Catalog No. Product Name Information Added
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. Dec 25 2019
S9521 Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. Dec 18 2019
S6739 MN 64 MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. Dec 09 2019
S6631 Belotecan (CKD-602) hydrochloride Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. Dec 09 2019
S8844 BRD0539 BRD0539 is a potent inhibitor of spCas9 which disrupts spCas9-DNA binding and exerts dose and temporal control of spCas9 in human cell lines. Nov 11 2019
S8880 Lobaplatin ( D-19466) Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent. It is a platinum complex with DNA alkylating activity. Nov 11 2019
S8843 AZD7648 AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases. Oct 30 2019
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells. Jul 31 2019
S6359 Purine Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A. May 16 2019
S6077 Cytidine 5′-triphosphate (disodium salt) Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases. Apr 03 2019
TGF-beta/smad
Catalog No. Product Name Information Added
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 08 2020
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 06 2019
S8772 LY 3200882 LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. Jan 09 2019
S1292 Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 μM. Oct 26 2018
S7959 SIS3 HCl SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways. Oct 20 2016
S7663 Ruboxistaurin HCl(LY333531 ) 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. Oct 10 2016
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. Apr 30 2015
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. Feb 02 2015
S7658 Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes. Nov 27 2014
S7530 Vactosertib  (TEW-7197, EW-7197) Vactosertib  (TEW-7197, EW-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. Nov 27 2014
GPCR & G Protein
Catalog No. Product Name Information Added
S6665 Sparsentan (PS-433540,RE-021,DARA) Sparsentan is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist. Jan 20 2020
S6639 BAY-545 BAY-545 is an A2B adenosine receptor antagonist with ic50 of 59 nM. Jan 20 2020
S6659 Rimegepant (BMS-927711,BHV-3000) Rimegepant is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM. Jan 15 2020
S6646 CPI-444 CPI-444 is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtypes. Dec 18 2019
S6633 AM 095 AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. Dec 18 2019
S6717 TCS-OX2-29 TCX-OX2-29 is a OX2R antagonist (pKi = 7.5) that exhibits >250-fold selectivity for hOX2R compared with hOX1R (IC50s = 40 nM and >10,000 nM, respectively). Nov 13 2019
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. Nov 06 2019
S6619 ABT 702 dihydrochloride ABT-702 is a novel, potent non-nucleoside Adenosine kinase inhibitor with an IC50 of 1.7 nM. It has oral activity in animal models of pain and inflammation. Oct 30 2019
S6552 CYM5541 CYM5541 is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM. Oct 23 2019
S6565 JK184 JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. Aug 28 2019
PTK
Catalog No. Product Name Information Added
S8848 TAS-120 TAS-120 is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 3.9 nM, 1.3 nM, 1.6 nM and 8.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4 respectively. Dec 19 2019
S8874 PLX5622 PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. Nov 06 2019
S6725 PCI 29732 PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. Oct 30 2019
S8832 Branebrutinib (BMS-986195) Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. Sep 11 2019
S6546 PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM). Sep 11 2019
S6539 ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively. Sep 11 2019
S6526 SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. Sep 11 2019
S6541 MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. Aug 08 2019
S8854 JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable MET kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant MET (2 and 3 nM IC50). Aug 08 2019
S6509 AG 494 AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM). Jul 31 2019
Epigenetics
Catalog No. Product Name Information Added
S8909 UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines. Jan 20 2020
S6655 WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. Dec 31 2019
S8785 A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency. Dec 31 2019
S6744 Inauhzin Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity. Dec 09 2019
S6758 I-CBP112 I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively. Dec 09 2019
S8766 AT1 AT1 is highly selective Brd4 degrader which is a designed molecule based on the crystal structures of MZ1 bound to BRD4 as well as models of VHL proteins. Nov 11 2019
S8574 BI 894999 BI894999 is a novel potent and selective BET inhibitor with IC50 values of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1. Nov 11 2019
S8297 ARV-825 ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC. Aug 08 2019
S6497 SMI-16a SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively. Jul 31 2019
S8743 SKLB-23bb SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. Jul 09 2019
NF-κB
Catalog No. Product Name Information Added
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 06 2019
S8642 GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases. Jul 03 2018
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. Nov 15 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
S7672 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2. Sep 14 2015
S7697 LY2409881 LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. Apr 20 2015
Metabolism
Catalog No. Product Name Information Added
S6666 FT113 FT113 is a potent inhibitor of fatty acid synthase(FASN) with ic50 of 213 nM. Jan 20 2020
S8847 BAY 2402234 BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM. Dec 31 2019
S8878 NDI-091143 NDI-091143 is a potent inhibitor of human ATP-citrate lyase(ACLY) with a Ki of 7.0 nM and an IC50 of 2.1 nM in the ADP-Glo assay. Dec 31 2019
S8895 Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM. Dec 18 2019
S6629 GNE-617 GNE-617 is a highly potent inhibitor of NAMPT activity with an IC50 of 5 nM. Dec 09 2019
S6728 IDO-IN-1 IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM. Dec 09 2019
S6626 Brequinar Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro. Nov 28 2019
S8563 TVB-3664 TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor. Nov 11 2019
S8881 DS-1001b (DS 1001, DS-1001) DS-1001 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) mutant forms, including substitution mutations at the arginine in position 132, IDH1(R132) (IDH1-R132), with potential antineoplastic activity. Nov 11 2019
S2933 AM580 AM580 is a retinoic acid receptor agonist with Kd values of 8 nM, 131 nM and 450 nM for RARα, RARβ and RARγ. Nov 06 2019
Proteases
Catalog No. Product Name Information Added
S8455 Talabostat (Val-boroPro, 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. Oct 23 2019
S6417 GK921 GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition. Apr 30 2019
S8778 UPGL00004 UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2. Mar 14 2019
S5611 2-cyano-Pyrimidine 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM. Mar 06 2019
S5909 Anagliptin Anagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. Jan 16 2019
S4956 Benzamidine HCl Benzamidine is an inhibitor of serine proteases with Ki values of 35, 350, and 220 µM for trypsin, plasmin, and thrombin, respectively. Jan 16 2019
S4997 4-Butylresorcinol 4-Butylresorcinol is a potent inhibitor of tyrosinase and is used in cosmetics as a depigmenting agent. Nov 28 2018
S5720 Glecaprevir Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a. Oct 18 2018
S5652 Elbasvir Elbasvir is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype. Sep 11 2018
S5365 Alogliptin Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. Aug 15 2018
Microbiology
Catalog No. Product Name Information Added
S4393 Cephapirin Sodium Cephapirin Sodium is the sodium salt form of cephapirin, a semi-synthetic, first-generation cephalosporin antibiotic with bactericidal activity.Cephapirin Sodium is effective against gram-negative and gram-positive organisms. Dec 19 2019
S4404 Pasiniazid Pasiniazid is a composition of isoniazid and 4-aminosalicylic acid, used to treat tuberculosis patients. Dec 19 2019
S6625 Temsavir (BMS-626529) Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses. Dec 09 2019
S6729 Besifovir Besifovir is novel and potent acyclic nucleotide phosphonate used to treat hepatitis B virus (HBV) infection. Oct 30 2019
S6581 Fosamprenavir calcium salt Fosamprenavir is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections. Sep 24 2019
S4421 Josamycin Josamycin is a macrolide antibiotic from Streptomyces narbonensis. The drug has antimicrobial activity against a wide spectrum of pathogens. Sep 11 2019
S6582 Ozenoxacin Ozenoxacin is a quinolone antibiotic used for the treatment of impetigo. Sep 11 2019
S8871 Omadacycline tosylate Omadacycline is a first-in-class aminomethylcycline antibiotic, demonstrating antimicrobial activity in vitro against a range of Gram-positive and Gram-negative aerobes and some anaerobic bacteria. Sep 05 2019
S6549 PBTZ169 PBTZ169, an antibiotic with antimycobacterial activity, is an irreversible inhibitor of DprE1. Aug 28 2019
S6562 KKL-35 KKL-35 inhibits the trans-translation tagging reaction with an IC50 of 0.9 µM. It has broad-spectrum antibiotic activity. Aug 28 2019
Apoptosis
Catalog No. Product Name Information Added
S6643 R-7050 R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β. Dec 11 2019
S8781 Selpercatinib (LOXO-292, ARRY-192) 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. Nov 13 2019
S8703 Milademetan (DS-3032b) Milademetan (DS-3032b) is a novel potent MDM2 inhibitor that inhibits MDM2-p53 interaction with an IC50 of 5.57 nM in the HTRF assay. Nov 11 2019
S8716 BLU-667 BLU-667 is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T). Oct 10 2019
S8865 BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM. Sep 17 2019
S8872 GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified. Sep 05 2019
S8864 ZT-12-037-01 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. Sep 05 2019
S8735 BI-3812 BI-3812 is a highly potent and efficacious BCL6 inhibitor probe compound with an IC50 less than 3 nM. Jul 31 2019
S6499 PF-6260933 PF-6260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. Jul 31 2019
S6511 RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor. Jul 24 2019
MAPK
Catalog No. Product Name Information Added
S6658 ETC-206 (AUM 001,ETC-1907206) ETC-206 is an orally available highly selective small-molecule MNK 1/2 inhibitor with IC50s of 64 nM and 86 nM, respectively. Jan 15 2020
S6660 B-Raf inhibitor 1 (Compound 13) dihydrochloride B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively. Jan 15 2020
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. Dec 09 2019
S8853 Belvarafenib(GDC5573, HM95573, RG6185) 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. Nov 19 2019
S8734 AZD7624 AZD7624 is a potent and selective competitive inhibitor against p38α/β with pIC50s of 10 and 8.8 for p38α and p38β respectively. Nov 11 2019
S6596 AG-126 AG126 is a tyrosine kinase inhibitor which selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM. Nov 06 2019
S6711 IQ-1S IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. Nov 06 2019
S6730 CC-401 Hydrochloride CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. Oct 30 2019
S8868 NG25 NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectively. Oct 10 2019
S8867 Bentamapimod (AS602801) Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. Aug 28 2019
Angiogenesis
Catalog No. Product Name Information Added
S6662 AST-487 (NVP-AST487) AST-487,a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. Jan 15 2020
S8882 ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively. Jan 08 2020
S8899 FF-10101 FF-10101 is a novel irreversible FLT3 inhibitor with ic50 of 0.20 nM and 0.16 nM for FLT3 (WT) and FLT3(D835Y), respectively. Dec 31 2019
S2934 Ensartinib (X-396) dihydrochloride Ensartinib (X-396) is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM. Dec 09 2019
S8814 TAS6417 TAS6417 is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L. Nov 19 2019
S2188 Phenprocoumon Phenprocoumon(Marcumar) is a vitamin K reductase with an IC50 of 1 μM Sep 09 2019
S6567 Src Inhibitor 1 Src Inhibitor 1 is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes. Aug 28 2019
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. Aug 08 2019
S6519 R112 R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM. Jul 24 2019
S6513 HG-14-10-04 HG-14-10-04 is an inhibitor of ALK. Jul 24 2019
Stem Cell & Wnt
Catalog No. Product Name Information Added
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). Nov 28 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. Oct 30 2019
S8704 iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay. Jul 09 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. Feb 20 2019
S8761 Adavivint (SM04690) SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays. Jan 23 2019
S5439 5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). Jul 12 2018
S8645 IWP-O1 IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells. Jun 01 2018
S8661 CA3(CIL56) 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 15 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 07 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 10 2018
Ubiquitin
Catalog No. Product Name Information Added
S8904 USP25/28 inhibitor AZ1 AZ1 is a potent and noncompetitive dual Inhibitors of the ubiquitin-specific protease (USP) 25/28 with IC50s of 0.62 μM and 0.7 μM in Ub-RH110 assay,respectively. Jan 15 2020
S6748 ML364 ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate. Nov 28 2019
S8341 TAK-243 (MLN7243) TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. May 16 2019
S5841 DKM 2-93 DKM 2-93 is a relatively selective lead inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5). Feb 27 2019
S5315 PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro. Jun 24 2018
S8696 2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. May 24 2018
S7109 Pevonedistat (MLN4924) MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM. Aug 31 2017
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro. May 19 2017
S7892 Avadomide(CC-122) Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN. Mar 31 2017
S4920 b-AP15 b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. Mar 30 2015
Neuronal Signaling
Catalog No. Product Name Information Added
S6644 Radiprodil (RGH-896) Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain. Dec 09 2019
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. Dec 09 2019
S6731 Eliprodil (SL-820715) Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 μM. Nov 06 2019
S6733 Edonerpic maleate Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). Oct 30 2019
S6618 JNJ-42153605 JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM. Oct 23 2019
S6583 Apraclonidine HCl Apraclonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist. Sep 11 2019
S3153 Levalbuterol tartrate Levalbuterol HCl is a relatively selective beta2-adrenergic receptor agonist used for the treatment of asthma. Sep 09 2019
S6592 Diquafosol Tetrasodium Diquafosol Tetrasodium, a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease. Sep 05 2019
S6612 Betazole Dihydrochloride Betazole Dihydrochloride is a histamine H2 agonist used clinically to test gastric secretory function. Aug 21 2019
S6569 VUF10460 VUF10460 is a histamine H4 receptor agonist. Aug 21 2019
Others
Catalog No. Product Name Information Added
S6663 Resmetirom (MGL-3196,VIA-3196) Resmetirom is a liver-directed, orally active, selective thyroid hormone receptor β(THR-β) agonist with an EC50 of 0.21 μM,shows 28-fold selective for THR-β over THR-α in a functional assay. Jan 20 2020
S6668 NVS-ZP7-4 NVS-ZP7-4,a Zinc transporter SLC39A7 (ZIP7) inhibitor,is the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway. Jan 20 2020
S8466 ST2825 ST2825,a synthetic peptido-mimetic compound,inhibits myeloid differentiation factor 88(MyD88) homodimerization in a TIR‐dependent manner and interferes with recruitment of IRAK1 and IRAK4 by MyD88. Jan 15 2020
S8923 AQX-435 AQX-435 is a novel SHIP1 activator. Jan 15 2020
S6651 G15 (GRB-G15) G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Jan 08 2020
S6657 2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations. Jan 08 2020
S8893 Firsocostat (GS-0976,NDI-010976,ND-630) Firsocostat is a reversible inhibitor of acetyl CoA carboxylase (ACC) with IC50s of 2.1 nM,6.1 nM for hACC1 and hACC2,respectively. Jan 08 2020
S8902 ERD-308 ERD-308 is a highly potent PROTAC degrader of Estrogen Receptor (ER) with DC50 of 0.17 nM in MCF-7 cell lines. Jan 08 2020
S8890 MK-8719 MK-8719 is a selective and potent small molecule inhibitor of the O-GlcNAcase (OGA) enzyme with ki of 7.9nM for hOGA. Jan 08 2020
S6637 HC-067047 HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. Dec 31 2019