“alpha ergocryptine”的搜索结果
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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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ABHD6 inhibitor
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.
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PKCδ inhibitor
BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM).
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PRMT5 inhibitor
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
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c-Src inhibitor
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
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PKC inhibitor
LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma.
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COX/LOX inhibitor
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 ?M??
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ACMSD inhibitor
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13??3 nM.
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dual PI3K and mTOR kinase inhibitor
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
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PI3Kδ inhibitor
Parsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
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dual TACE/MMPs inhibitor
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) .
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ACCA inhibitor
TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
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multi-targeted tyrosine kinase inhibitor
Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
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caspase inhibitor
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 ?M.
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p38 MAPK inhibitor
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity.
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p38 MAP kinase inhibitor
Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.385.42
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multi-targeted tyrosine kinase inhibitor
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret.
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KGDHC inhibitor
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts.
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multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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Hydroxy aryl aldehydes (HAA) inhibitor
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
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p38 MAP kinase inhibitor
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).
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Akt inhibitor
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
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PKC inhibitor
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively.
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PIP5K?? inhibitor
ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects .
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HIF-1?? inhibitor
AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
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HSP90??/HSP90?? inhibitor
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
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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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