New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
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
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
JAK/STAT
Catalog No. Product Name Information Added
S2275 Gandotinib (LY2784544) Gandotinib is a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase with IC50 of 3 nM. Gandotinib may have the potential to effectively reduce the JAK2V167F-induced MPN pathogenesis. Apr 02 2020
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
Cell Cycle
Catalog No. Product Name Information Added
S8955 AMG-510 racemate AMG-510 racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. Mar 18 2020
S1058 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM. Mar 11 2020
S8884 MRTX849 MRTX849 is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling. Mar 04 2020
S6673 CCG-222740 CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression. Feb 28 2020
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
DNA Damage
Catalog No. Product Name Information Added
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
S6692 RG7800 RG7800 can modify the alternative splicing of SMN2, increasing the production of fulllength SMN2 mRNA. RG7800 is a first small molecule SMN2 splicing modifier to enter human clinical trials. Mar 06 2020
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
TGF-beta/smad
Catalog No. Product Name Information Added
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 05 2020
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM. Mar 04 2020
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
GPCR & G Protein
Catalog No. Product Name Information Added
S8938 KGA-2727 KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models. Apr 02 2020
S8939 Mizagliflozin Mizagliflozin is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation. Apr 02 2020
S6770 TT-OAD2 TT-OAD2 is a biased non-peptide agonist with slow kinetics. TT-OAD2 can activate the glucagon-like peptide-1 (GLP-1) receptor. Mar 17 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
S6693 MRS 1754 MRS 1754 is a selective antagonist ligand of A2B adenosine receptors, with very low affinity for A1 and A3 receptors of both humans and rats. Mar 06 2020
S6694 Grapiprant (CJ-023423) Grapiprant is the first EP4 receptor-specific antagonist approved by FDA for control of pain and inflammation in dogs with osteoarthritis. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor in a concentration-dependent manner with an IC50 value of 35 nM and with a Ki value of 24 nM. Mar 06 2020
S6695 AB928 (A2aR/A2bR antagonist-1) AB928 is a novel dual A2aR/A2bR antagonist. AB928 inhibits A2aR and A2bR with similar potencies(equilibrium binding constant of 1.4 and 2 nM, respectively). Mar 06 2020
S6649 E7046(ER-886406) E7046 is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM. Feb 12 2020
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
PTK
Catalog No. Product Name Information Added
S6514 SU5408 SU5408 is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM. Mar 25 2020
S2115 RG 13022 RG-13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM. Mar 17 2020
S2070 ISCK03 ISCK03 is a cell-permeable inhibitor of stem-cell factor (SCF)/c-kit signaling.ISCK03 inhibits SCF-induced c-c-kit phosphorylation and downstream ERK phosphorylation. Mar 11 2020
S1054 AG99 AG99 is a potent and selective inhibitor of EGFR. Mar 11 2020
S6760 LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro. Mar 09 2020
S6762 Bozitinib (PLB-1001) Bozitinib is a highly selective ATP-competitive small-molecule c-Met inhibitor with blood-brain barrier permeability. Mar 09 2020
S6763 Acrizanib (LHA510) Acrizanib is an inhibitor of VEGFR-2 with IC50 of 17.4 nM in BaF3-Tel-KDR cells. Mar 09 2020
S6764 TAS-115 TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively. Mar 09 2020
S6698 TQB3804 (EGFR-IN-7) TQB3804 is a selective and potent EGFR kinase inhibitor, has IC50 values of 7.92 nM,0.218 nM and 0.16 nM for EGFR(WT), EGFR(19del/T790M/C797S) and EGFR(L858R/T790M/C797S) respectively, and shows anti-tumor activity. Mar 06 2020
S2211 AG-13958 AG–013958, a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD). Mar 04 2020
Epigenetics
Catalog No. Product Name Information Added
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
S8952 iRucaparib-AP6 iRucaparib-AP6 is a potent and selective small-molecule degrader of PARP1. iRucaparib-AP6 blocks the enzymatic activity of PARP1 in vitro, and PARP1-mediated poly-ADP-ribosylation signaling in intact cells. Mar 17 2020
S2184 WDR5-0103 WDR5-0103 is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM. Mar 11 2020
S6682 Bobcat339 Bobcat339 is a selective cytosine-based TET enzyme inhibitor with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 can reduce DNA 5-hydroxymethylcytosine abundance by inhibiting TET enzyme function in living cells and provide support for its utility as a viable pharmacological probe. Mar 11 2020
S6696 EZM 2302 (GSK3359088) EZM2302 is an inhibitor of CARM1 enzymatic activity in biochemical assays(IC50 = 6 nM) with broad selectivity against other histone methyltransferases. Mar 06 2020
NF-κB
Catalog No. Product Name Information Added
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
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). Mar 25 2020
S8941 NIK SMI1 NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP. Mar 25 2020
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
Metabolism
Catalog No. Product Name Information Added
S2274 TMS TMS is a potent, selective and competitive cytochrome P450 1B1 (CYP1B1) inhibitor with IC50 of 6 nM. TMS exhibits 50-fold selectivity for P450 1B1 over P450 1A1 with IC50 of 300 nM and 500-fold over P450 1A2 with IC50 of 3 μM. Apr 02 2020
S2419 Eprobemide Eprobemide is a reversible monoamine oxidase A (MAO-A) inhibitor. Eprobemide acts as an antidepressant in Russia. Apr 02 2020
S2421 PF-04457845 PF-04457845 is a potent, favorable selective inhibitor of Fatty acid amide hydrolase (FAAH) with IC50 of 7.2 nM and 7.4 nM for hFAAH and rFAAH, respectively. PF-04457845 covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily. Apr 02 2020
S6689 Merimepodib Merimepodib is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent. Mar 25 2020
S8949 Olutasidenib (FT-2102) Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively. Mar 25 2020
S6681 Paricalcitol Paricalcitol is a selective vitamin D receptor agonist. Paricalcitol suppresses parathyroid hormone mRNA expression and inhibits parathyroid cell proliferation. Pariccitol is used to treat secondary hyperparathyroidism in chronic kidney disease. Mar 11 2020
S6690 TOFA (5-(Tetradecyloxy)-2-furoic acid) TOFA is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA). Inside the cell, TOFA is converted to TOFyl-CoA (5-tetradecyloxy-2-furoyl-CoA), exerting an allosteric inhibition on ACCA. TOFA blocks fatty acid synthesis and induces cell death in a dose-dependent manner. Mar 11 2020
S1024 LTI-291 LTI-291 is the first small-molecule activator of Glucocerebrosidase(GCase) for the treatment of parkinson's disease. Mar 11 2020
S6635 Seladelpar sodium (MBX-8025 sodium) MBX-8025 is an orally active, potent and selective agonist of PPAR-δ with an EC50 of 2 nM. MBX-8025 exhibits more than 750-fold, 2500-fold selectivity over PPAR-α and PPAR-γ receptors, respectively. Mar 11 2020
S8377 ND646 In cell-free systems, ND-646 inhibits the enzymatic activity of recombinant human ACC1 (hACC1) and recombinant hACC2 with IC50 of 3.5 nM and 4.1 nM, respectively. Mar 09 2020
Proteases
Catalog No. Product Name Information Added
S8891 JHU-083   Feb 12 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. 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
Microbiology
Catalog No. Product Name Information Added
S2430 Azodicarbonamide Azodicarbonamide is the first known nucleocapsid inhibitor that inhibits HIV-1 and a broad range of retroviruses by targeting the nucleocapsid CCHC domains. Azodicarbonamide inhibits the HIV-1RF-induced cytopathicity of CEM-SS cells with an EC50 of 38 µM in a standard cell-based antiviral assay . Apr 02 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. Mar 17 2020
S8932 Remdesivir (GS-5734) Remdesivir,a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. Mar 12 2020
S6761 Dalfopristin Dalfopristin is a semi-synthetic analogue of ostreogyrcin A, Quinupristin/dalfopristin is a new combination streptogramin product with a selective spectrum of antibacterial activity, mainly against gram-positive aerobic bacteria. Mar 09 2020
S6676 Ebselen Ebselen is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay. Feb 28 2020
S9466 Methenamine Hippurate Methenamine Hippurate is the hippurate salt form of methenamine, a prodrug and inactive weak base that is hydrolyzed to formaldehyde in acid urine.Methenamine Hippurate is the component of Hiprex drug which has antibacterial activity. Feb 12 2020
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
Apoptosis
Catalog No. Product Name Information Added
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
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) 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
MAPK
Catalog No. Product Name Information Added
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
S8569 KO-947 KO-947 is a potent and selective ERK1/2inhibitor.KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations. Mar 09 2020
S6641 GW284543 (UNC10225170) GW284543 is a MEK5-selective inhibitor. GW284543 can dose dependently inhibits MEK5 by reduces in pERK5 and decreases endogenous MYC protein. Mar 06 2020
S6658 ETC-206 (AUM 001) 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 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
Angiogenesis
Catalog No. Product Name Information Added
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
S8948 SRX3207 SRX3207 is a novel dual Syk-PI3K inhibitor with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 can relieve tumor immunosuppression. Mar 09 2020
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
Stem Cell & Wnt
Catalog No. Product Name Information Added
S8392 NCB-0846 NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase) with an IC50 value of 21 nM. Mar 12 2020
S6699 Gigantol Gigantol is a novel small-molecule Wnt/β-catenin inhibitor, gigantol has been shown to have promising therapeutic potential in cancer cells. Mar 06 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 04 2020
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
Ubiquitin
Catalog No. Product Name Information Added
S6640 GNE-6640 GNE­6640 selectively inhibits recombinant ubiquitin epecific peptidase 7(USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP47 and Ub-MDM2, respectively. Mar 06 2020
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
Neuronal Signaling
Catalog No. Product Name Information Added
S2434 IDRA-21 IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability. Apr 02 2020
S2418 Frentizole Frentizole is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. Apr 02 2020
S2464 Sevoflurane Sevoflurane is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics. Apr 02 2020
S2644 Lerisetron Lerisetron is a 5-HT3 receptor antagonist with IC50 of 0.81μM. Apr 02 2020
S2645 SIB 1757 SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8. Apr 02 2020
S6664 Gefapixant Gefapixant is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough. Mar 11 2020
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
Others
Catalog No. Product Name Information Added
S2428 Isopropyl myristate Isopropyl myristate is used as a substitute for natural oils in cosmetics and a co-solvent with skin penetration enhancement properties of active ingredients in many topical and transdermal preparations. Isopropyl myristate is a novel pediculicide rinse (50%) and a safe and effective therapy for the treatment of head lice in children and adults. Apr 02 2020
S2429 2-Ethylaniline 2-Ethylaniline is an intermediate for pharmaceuticals, dyestuffs, pesticides, and other products. Apr 02 2020
S8944 G150 G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with IC50 of 10.2 nM. Apr 02 2020
S2474 Fabomotizole hydrochloride Fabomotizole hydrochloride exhibits anxiolytic and neuroprotective properties. Fabomotizole hydrochloride is a potent sigma1-receptor agonist with IC50 of 7.1 µM and Ki of 5.9 µM. Apr 02 2020
S2488 VTP-27999 TFA VTP-27999 is an orally efficacious, selecitive alkyl amine renin inhibitor with IC50 of 0.47 nM for 0.3 nM of purified recombinant human renin. Apr 02 2020
S2432 Tetramethylthiuram monosulfide Tetramethylthiuram monosulfide is used on a large scale as a catalyst in rubber-processing techniques. Tetramethylthiuram monosulfide possesses a medium-degree toxicity and causes point mutations in strains TA 100 and TA 1535 (Salmonella typhimurium LT 2). Apr 02 2020
S8913 TH5487 TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM. Apr 02 2020
S2426 Tirapazamine Tirapazamine is a new anticancer drug in solid tumours. Tirapazamine exhibits preferential tumour cell killing and high specific toxicity to cells at low oxygen tensions. Apr 02 2020
S2436 Pranidipine Pranidipine is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta. Apr 02 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