Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。 了解更多

Celecoxib是一种磺胺类非甾体抗炎药（NSAID）和选择性COX-2抑制剂，在Sf9细胞中IC50为40 nM。 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

Celgosivir是一种用于潜在治疗HCV感染的α-葡萄糖苷酶I抑制剂。 了解更多

EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration. 了解更多

Briciclib disodium salt是苄基苯乙烯基砜类似物，是ON 013100的磷酸二钠酯前药物，具有潜在的抗肿瘤活性。 了解更多

Dasatinib hydrochloride是一种有效的Abl/Src双重抑制剂，IC50分别<1 nM/0.8 nM。还可以抑制c-Kit（WT/c-Kit（D816V），IC50为79 nM/37 nM。有效，选择性Raf激酶抑制剂能够抑制野生型B-Raf，B-RafV600E和c -Raf的IC50值分别为3.2、0.8和5.0 nM。 了解更多

NG52 (Compound 52)是细胞周期调节激酶Cdc28p（IC50 = 7 μM）和相关Pho85p激酶（IC50 = 2 μM）的有效，可渗透细胞，可逆，选择性和ATP兼容的抑制剂。 了解更多

K-7174是一种新型的细胞粘附抑制剂；抑制由IL-1beta或TNF-alpha诱导的血管细胞粘附分子1（VCAM-1）的表达。 了解更多

K-7174 dihydrochloride是一种新型的细胞粘附抑制剂；抑制由IL-1beta或TNF-alpha诱导的血管细胞粘附分子1（VCAM-1）的表达。 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

ON-013100是细胞周期抑制剂，可能可用于治疗套细胞淋巴瘤。 了解更多

AX-024是一种细胞因子释放抑制剂，可以强烈抑制白介素6（IL-6），肿瘤坏死因子-α（TNFα），干扰素-γ（IFN-γ），IL-10和IL-17A的产生。 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

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

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

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

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

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

BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM. 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

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

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

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

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM. 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

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

SSE15206 is a pyrazolinethioamide derivative that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents. 了解更多

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

Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay. 了解更多

Nerolidol is a synthetic AChE inhibitor and F0F1-ATP synthase modulator. It acts as a sedative, inhibits growth of bacteria and fungi, and decreases the mitochondrial transmembrane electric potential to induce cell death in hepatocarcinoma cells. 了解更多

Deracoxib is an NSAID and COX-2 inhibitor used to treat osteoarthritis. It induces cell cycle arrest and apoptosis in mammary tumor cells, decreases platelet aggregation, and lowers inflammatory responses. 了解更多

Fosfomycin calcium is a MurA and isopentenyl mevalonate kinase inhibitor that prevents synthesis of bacterial cell walls. 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

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

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

ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. 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

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

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

TVB-3166 is an orally-available, reversible, potent, and selective FASN inhibitor, inducing apoptosis, inhibiting anchorage-independent cell growth under lipid-rich conditions, and inhibiting in-vivo xenograft tumor growth. 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

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

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

ARN-3236 is potent, orally active and selective SIK2 inhibitor. ARN-3236 inhibited the growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μmol/L. 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

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

D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D 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