“alpha ergocryptine”的搜索结果
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Alpha-galactosidase 抑制剂
Deoxygalactonojirimycin Hydrochloride是一种有效且选择性的Alpha-gal A(Alpha-半乳糖苷酶)抑制剂。
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α9β1/α4β1 integrin 抑制剂
BOP sodium salt是新型的双重alpha9beta1/alpha4beta1整联蛋白抑制剂。
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α4β1/α9β1 抑制剂
R-BC154是高亲和力的荧光α4β1/α9 9β1抑制剂。
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platelet adhesion inhibitor
Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.
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alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
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5 alpha-reductase inhibitor
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.
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p38α MAPK inhibitor
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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oral α and β tubulin inhibitor
VERU-111 is a novel, oral α and β tubulin inhibitor that blocks tubulin polymerization and is not a substrate for multi-drug resistance mechanisms.
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PI3Kα/δ inhibitor
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
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MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
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TNFα inhibitor
C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
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IRE1α inhibitor
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
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HIF-1α/von Hippel-Lindau interaction inhibitor
ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M.
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IRE1α RNase kinase inhibitor
KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 ?M. KIRA6 can trigger an apoptotic response.
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IRE1α inhibitor
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
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PGF2α/LTB4 production inhibitor
Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
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α-glucoside hydrolase inhibitor
Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
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HIF1α inhibitor
EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
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p38α inhibitors
R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.
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HIF-2α inhibitor
(Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
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GSK-3α/β inhibitor
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
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GSK-3α/β inhibitor
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM.
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testosterone 5-alpha-reductase inhibitor
Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor.
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HIF-2α inhibitor
PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
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eukaryotic DNA polymerase α inhibitor
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM.
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triazole DAGL(α) inhibitor
DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
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p38α MAPK inhibitor
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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p38α MAPK inhibitor
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
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p38α MAPK inhibitor
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM.
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p38 MAPK α/β inhibitor
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively.
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α4 integrin receptor inhibitor
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
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αVβ3 integrin inhibitor
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
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adrenergic receptor inhibitor
Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
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PI3Kα 抑制剂
PI3K-alpha inhibitor 1 是从专利US/20120088764A1中提取的PI3Kα抑制剂,化合物243,IC50 <0.1uM,PI3Kα抑制剂1还抑制HDAC(0.1uM≤IC50≤1uM)。
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p53 抑制剂
Pifithrin-alpha是p53介导的细胞凋亡和p53依赖性基因转录(如细胞周期蛋白G,p21/waf1和mdm2表达)的可逆抑制剂。
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aromatase inhibitor
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
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Topoisomerase I inhibitor
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker.
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MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
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TNF-alpha 抑制剂
Pomalidomide (CC-4047)是沙利度胺的衍生物,在PBMCs中IC50为13 nM,并起免疫调节剂的作用。
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5-alpha reductase 抑制剂
β-Sitosterol是一种植物甾醇,与胆固醇具有相似的化学结构。
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HSP90 抑制剂
CUDC-305 (DEBIO-0932) 是一种新型的热休克蛋白90(HSP90)抑制剂,对HSP90 alpha/beta具有很强的亲和力,对HSP90α和HSP90β的IC50值分别为100和103nM。具有很高的口服生物利用度,并且对多种癌细胞系均具有强大的抗增殖活性(平均IC50为220 nmol/L)。包括许多对护理标准(SOC)药物有抵抗力的非小细胞肺癌(NSCLC)细胞系。
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- Aykut Ozgur, .et al. Debio-0932, a second generation oral Hsp90 inhibitor, induces apoptosis in MCF-7 and MDA-MB-231 cell lines, Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319
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alpha-glucosidase I 抑制剂
Celgosivir是一种用于潜在治疗HCV感染的α-葡萄糖苷酶I抑制剂。
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SERCA 抑制剂
Cyclopiazonic acid是SERCA(内质网Ca2+ -ATPase)的抑制剂,可诱导细胞内储存的Ca2+释放,而不会增加IP3水平。
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alpha-glucosidase 抑制剂
Voglibose是缬氨酰胺的N取代衍生物,对α-葡萄糖苷酶具有出色的抑制活性,并且对高血糖症和由高血糖症引起的各种疾病具有抗药性。
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mTOR 抑制剂
CC-223是一种有效的mTOR激酶抑制剂(IC50 = 16 nM),其敏感性是相关脂质激酶PI3K-alpha(IC50 = 4 uM)的> 150倍。
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PGC-1α 抑制剂
SR 18292是PGC-1α抑制剂。在T2D的饮食和遗传小鼠模型中,它可降低血糖,强烈提高肝胰岛素敏感性并改善葡萄糖稳态。
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α2β1 integrin 抑制剂
BTT-3033是α2β1整联蛋白抑制剂。
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α1β1 抑制剂
Obtustatin是高度有效的整联蛋白α1β1抑制剂(α1β1与IV型胶原的结合的IC 50 = 0.8 nM)。与α2β1,βIIbβ3,αvβ3,α4β1,β5β6,α9β1和α4β7相比,α1β1具有选择性。在鸡绒膜尿囊炎模型中抑制FGF2刺激的血管生成。在Lewis肺癌的协同小鼠模型中显示抗肿瘤功效;阻止人黑素瘤在裸鼠中的生长。
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CDK9 inhibitor
MC180295 is a highly selective CDK9 inhibitor (IC50 = 5 nM). MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
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ABHD6 inhibitor
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.
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