AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. 了解更多

Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells. 了解更多

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM. 了解更多

LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity. 了解更多

NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays. 了解更多

SIS17 is a potent and selective HDAC 11 inhibitor with an IC50 value of 0.83 μM. SIS17, is active in cells and inhibited the demyristoylation of a known HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. 了解更多

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity. 了解更多

BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity. 了解更多

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells. 了解更多

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells. 了解更多

JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages. 了解更多

INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells. 了解更多

KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells. 了解更多

KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells. 了解更多

MK-8719 is a highly potent and selective OGA inhibitor (EC50 = 52.7 nM) which is a Potential Treatment for Tauopathies. MK-8719 showed excellent CNS penetration that has been advanced to first-in-human phase I clinical trials. 了解更多

GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. 了解更多

WJ460 is an inhibitor of myoferlin (MYOF) which exerts anti-metastatic activity in the nanomolar range in breast cancer cells. 了解更多

Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells. 了解更多

Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells. 了解更多

Ras-IN-3144 is a pan-RAS inhibitor which inhibits RAS signaling pathways in cancer cells and prevents the growth of RAS mutant mouse cancer xenografts. 了解更多

MRTX1257 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, MRTX1257 inhibited KRAS dependent ERKphosphorylation in the H358cell assay with an IC50= 900 pM. 了解更多

SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected. 了解更多

Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis. 了解更多

JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. 了解更多

Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells. 了解更多

GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro. 了解更多

ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties. 了解更多

LY3000328 is a Cathepsin S inhibitor with excellent in vitro potency and selectivity against other cysteine proteases. 了解更多

RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. 了解更多

Mycophenolate mofetil (CellCept)是嘌呤生物合成（特别是鸟嘌呤合成）中肌苷单磷酸脱氢酶（IMPDH）的可逆抑制剂，对T细胞和B细胞的生长是必需的。 了解更多

KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life. 了解更多

AS601245 is a cell-permeable JNK Inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. 了解更多

CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM). 了解更多

Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5 ?M; Histone Acetyltransferase Inhibitor II can be used in cancer research. 了解更多

YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. 了解更多

PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM. 了解更多

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM. 了解更多

NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability. 了解更多

AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. 了解更多

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1. 了解更多

AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM). Inhibiting an immediate TCR signal has promise for treating a broad spectrum of human T cell-mediated autoimmune and inflammatory diseases. 了解更多

2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). 了解更多

GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 reduces apoptosis. 了解更多

Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle. 了解更多

Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. 了解更多

CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation. 了解更多

Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell. 了解更多

(R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132. 了解更多

PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). 了解更多