About 30 results found for searched term "STAT5-IN-2" (0.09 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M10968 | STAT5-IN-2 | STAT |
| STAT5-IN-2 is an inhibitor of STAT5 in K562 and KU812 cells EC50 9 μM and 5 μM respectively, the name in Document 1 is 17f. STAT5-IN-2 has highly effective antileukemia activity. | ||
| M1791 | Entinostat (MS-275) | HDAC |
| SNDX-275, MS-27-275 | ||
| Entinostat (MS-275) is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively. | ||
| M2126 | Fluvastatin sodium | HMG-CoA Reductase |
| XU 62-320 | ||
| Fluvastatin sodium is an orally active, potent and competitive HMG-CoA reductase inhibitor with IC50 value between 40 and 100 nM at human liver microsomes. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway. | ||
| M2315 | Necrostatin-1 | RIPK |
| Nec-1 | ||
| Necrostatin-1 (NEC-1) is a potent inhibitor of necroptosis, with an EC50 of 490 nM in Jurkat cells. Necrostin-1 is the first identified RIPK1 inhibitor, EC50=182 nM, that reduces inflammation and inhibits colitis associated tumorigenesis. Necrostatin-1 (Nec-1) is also an inhibitor of IDO. | ||
| M2537 | Cobicistat | Cytochrome P450 (e.g. CYP17) |
| GS-9350 | ||
| Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM. | ||
| M2829 | Marimastat | MMP |
| BB2516; TA2516 | ||
| Marimastat (BB-2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. | ||
| M2945 | Pimozide | Dopamine Receptor |
| R6238 | ||
| Pimozide is an antagonist of 6-hydroxyapatide against 6-hydroxyapatide, with Ki values of 1.4 nM, 2.5 nM and 588 nM for 6-hydroxyapatide, D3 and D1 receptors, respectively. Pimozide also has a high affinity for α1-adrenoceptor. Ki value is 39 nM. Pimozide is also an inhibitor of STAT3 and STAT5, and piperimidate triggers ADCD in glioblastoma cell lines (LN-229, MZ-54, GOS-3 and U343) by inducing dephosphorylation and inactivation of mTORC1. | ||
| M3032 | Stattic | STAT |
| Stattic is the first nonpeptidic STAT3 inhibitor, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1. Stattic inhibits STAT3 phosphorylation (at Y705 and S727). | ||
| M5795 | Molidustat (BAY 85-3934) | HIF |
| BAY 85-3934 | ||
| Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. | ||
| M7500 | YK 3-237 | Sirtuin |
| YK 3-237 is a boronic acid chalcone analog of combretastatin a4 (CA-4) and a SIRT1 activator that targets mutant p53. YK 3-237 can reduce the acetylation of mutant p53 protein by activating the SIRT1 enzyme, resulting in a significant decrease in the level of mutant p53 protein. YK-3-237 showed antiproliferative activity against tumor cells containing mutant p53 protein. | ||
| M8299 | Methylstat | Others |
| Methylstat is an inhibitor of the Jumonji C domain-containing histone trimethyl demethylases (JHDMs). Methylstat inhibits the activity of JMJD2C (IC50 = 4.3 μM), with similar potency against JMJD2E and JMJD3. | ||
| M9077 | STAT5-IN-1 | STAT |
| STAT5 Inhibitor | ||
| STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform. STAT5-IN-1 is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain. | ||
| M9198 | JTZ-951 | HIF |
| Enarodustat | ||
| Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. | ||
| M10534 | Tucidinostat (Chidamide) HCl | HDAC |
| Chidamide; HBI-8000; CS-055 HCl | ||
| Tucidinostat (HBI-8000; Chidamide; CS-055) HCl is a benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10 with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. | ||
| M10727 | Pulrodemstat benzenesulfonate | Histone demethylase |
| CC-90011 benzenesulfonate | ||
| CC-90011 (Pulrodemstat) benzenesulfonate is a potent, selective, reversible and orally active lysine-specific demethylase-1 (LSD1) inhibitor,IC50 0.25 nM. CC-90011 benzenesulfonate has less enzymatic inhibition of LSD2, MOA-A and MAO-B. CC-90011 benzenesulfonate induces differentiation of acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells and has potent anti-cancer activity. | ||
| M11253 | BD750 | JAK |
| BD750 is an effective immunosuppressant of JAK3/STAT5 and inhibits IL-2-induced JAK3/ STAT5-dependent T cell proliferation with IC50 values of 1.5 μM and 1.1 μM in mice and human T cells, respectively. | ||
| M11294 | Alicapistat | Proteasome |
| ABT-957 | ||
| Alicapistat (ABT-957) is an orally active, selective inhibitor of human calpains 1 and 2 that can be used in alzheimer's disease (AD) studies. | ||
| M13406 | Deacetylase Inhibitor Cocktail (100X) | Inhibitor Cocktails |
| AbMole Deacetylase Inhibitor Cocktail is a synergistic combination of chemicals designed to preserve the acetylation state of proteins. AbMole Deacetylase Inhibitor Cocktail (100X) is provided as 1 mL vial. Each vial contains 1 mL 70% DMSO with the following components: Trichostatin A (40 μM), EX-527 (1 mM), Nicotinamide (400 mM), and Sodium Butyrate (200 mM). | ||
| M13556 | Necrostatin 2 | RIPK |
| Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor. | ||
| M14069 | Numidargistat dihydrochloride | Others |
| CB-1158 dihydrochloride; INCB01158 dihydrochloride | ||
| Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase, with IC50s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent. | ||
| M58604 | Vipoglanstat | PGE synthase |
| BI 1029539; GS-248; OX-MPI | ||
| Vipoglanstat (BI 1029539) is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = ≤0.5 nM in isolated human whole blood). Vipoglanstat reduces LPS-induced increases in the influx of neutrophils and levels of cytokines in bronchoalveolar lavage fluid (BALF), as well as the expression of PTGES, the gene encoding mPGES-1, Cox2, and Icam1 in the lung parenchyma, in a human PTGES knock-in mouse model of acute lung injury when administered at a dose of 30 mg/kg. | ||
| M14148 | STAT3-IN-1 | STAT |
| STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis. | ||
| M20389 | Quisinostat (JNJ-26481585) 2HCl | HDAC |
| Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11 greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2. | ||
| M21184 | Soticlestat | Cytochrome P450 (e.g. CYP17) |
| TAK-935; OV935 | ||
| Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, orally active inhibitor of cholesterol 24-hydroxylase (CH24H), which is used in the study of epilepsy syndromes. | ||
| M27608 | BMS-593214 | Others |
| BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT). | ||
| M27865 | Histatin 5 | MMP |
| Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively. | ||
| M28215 | IST5-002 | STAT |
| N6-Benzyladenosine-5'-phosphate | ||
| IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML). | ||
| M28540 | Talabostat | Dipeptidyl Peptidase |
| Val-boroPro; PT100 | ||
| Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities. | ||
| M29365 | Dazcapistat | Proteasome |
| Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively. | ||
| M29517 | Pomstafib-2 | STAT |
| Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis. | ||
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