Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL. 了解更多

T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes. 了解更多

Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma. 了解更多

ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5?nM. 了解更多

Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature. 了解更多

5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 了解更多

CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform. 了解更多

SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. 了解更多

ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations. 了解更多

RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. 了解更多

Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. 了解更多

RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity. 了解更多

RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively. 了解更多

MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors. 了解更多

ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively. 了解更多

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM. 了解更多

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer??s disease. 了解更多

P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. 了解更多

Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis. 了解更多

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer??s disease. 了解更多

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. 了解更多

PXS-5153A is a novel mechanism based, fast-acting, dual LOXL2/LOXL3 inhibitor, which was used to interrogate the role of these enzymes in models of collagen crosslinking and fibrosis. 了解更多

PF-4191834 is a novel, potent and selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain with an IC50=229 nM. displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes. 了解更多

Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. 了解更多

Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon. 了解更多

Sodium Dichloroacetate, also known as CPC-211; DCA; X-11S, is a Pyruvate dehydrogenase kinase inhibitor potentially for the treatment of myocardia ischemia, ischemic. Sodium dichloroacetate also exhibits anti-leukemic activity in B-chronic lymphocytic leukemia (B-CLL) and synergizes with the p53 activator Nutlin-3. Sodium dichloroacetate (DCA) reduces apoptosis in colorectal tumor hypoxia. 了解更多

Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9. 了解更多

Acetylglucosamine or N-acetylglucosamine is potentially for the treatment of irritable bowel syndrome. N-Acetylglucosamine (GlcNAc) is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. GlcNAc has been reported to be an inhibitor of elastase release from human polymorphonuclear leukocytes (range 8?C17% inhibition), however this is much weaker than the inhibition seen with N-acetylgalactosamine (range 92?C100%). 了解更多

Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor. 了解更多

Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles. 了解更多

Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression. 了解更多

Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin. 了解更多

Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. 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

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

Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively). 了解更多

TMI-1是ADAM17（TACE）和MMP的新型活性双重抑制剂。 了解更多

Pyrotinib Racemate是吡罗替尼的外消旋体。吡罗替尼是一种有效的选择性EGFR/HER2双重抑制剂。 了解更多

MLN-4760是血管紧张素转化（ACE2）抑制剂。在huMNC中，MLN-4760-B检测到63％的ACE2，选择性是ACE的28倍。 了解更多

WM-1119是赖氨酸乙酰基转移酶KAT6A的高效选择性抑制剂，IC50为0.25 uM。它对KAT6A的活性分别是对KAT5或KAT7的1100倍和250倍。 了解更多

STO-609是钙/钙调蛋白依赖性激酶激酶（CaMKK）亚型CaMKKα和CaMKKβ（Ki分别为80和15 ng/ml）的细胞渗透性抑制剂。 了解更多

(S)-Gossypol acetic acid是Bcl-2的抑制剂，在过表达Bcl-2（IC50，18.1μM）或Bcl-xL（IC50，22.9μM）的Jurkat细胞中有效诱导细胞死亡。 了解更多

AZ505 ditrifluoroacetate是一种有效且高度选择性的致癌蛋白SMYD2抑制剂（IC50 = 0.12 uM），具有潜在的抗癌活性，是SMYD3的> 600倍（IC50> 83.3 uM）。DOT1L（IC50> 83.3 uM）；EZH2（IC50> 83.3 uM）。 了解更多

Verubecestat (MK-8931)是一种有效的选择性β-分泌酶抑制剂，是BACE1蛋白抑制剂或Beta-site APP裂解酶1抑制剂。 了解更多

Hexa-D-arginine是弗林蛋白酶的抑制剂（弗林蛋白酶，PACE4和PC1的Ki值分别为0.106、0.58和13.2 uM）。 了解更多

Nelfinavir是一种有效的口服生物可利用的人类免疫缺陷病毒HIV-1蛋白酶抑制剂(Ki=2 nM ),广泛用于与HIV逆转录酶抑制剂联合治疗HIV感染。 了解更多

M344是HDAC的有效抑制剂，IC50为100 nM，能够诱导细胞分化。 了解更多

Begacestat (GSI-953)是一种新型的选择性淀粉样前体蛋白γ-分泌酶的噻吩磺酰胺抑制剂。 了解更多