About 30 results found for searched term "STAT5-IN-1" (0.087 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M9077 | STAT5-IN-1 | STAT |
| STAT5 Inhibitor | ||
| STAT5-IN-1 is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain, with an IC50 of 47 μM for STAT5β isoform. | ||
| 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. | ||
| M9217 | Givinostat | HDAC |
| ITF2357 | ||
| Givinostat (ITF-2357) is an HDAC inhibitor with IC50s of 198 and 157 nM for HDAC1 and HDAC3, respectively. | ||
| 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. | ||
| 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. | ||
| M3095 | Tubastatin A | HDAC |
| Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). | ||
| M5259 | Citarinostat | HDAC |
| ACY-241 | ||
| Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. | ||
| 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. | ||
| M6603 | Cilastatin sodium | Anti-infection |
| Cilastatin sodium is a reversible, competitive renal dehydropeptidase I inhibitor with IC50 of 0.1 μM, it inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. | ||
| 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. | ||
| M7647 | Bryostatin 1 | PKC |
| Bryostatin 1 is a natural macrolide isolated from the moss bug Bugula neritina and a potent PKC modulator of central nervous system (CNS) permeability.Bryostatin 1 binds to the isolated Munc13-1 C1 domain and the full-length Munc13-1 protein with a Ki value of 8.07 and 0.45 nM, respectively, and has anticancer, anti-inflammatory and neuroprotective activities. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Ki values of 8.07 nM and 0.45 nM, respectively, and exhibits anticancer, anti-inflammatory, and neuroprotective activities. | ||
| M7942 | Necrostatin-5 | RIPK |
| Necrostatin-5 is an inhibitor of necroptosis (non-apoptotic cell death pathway) by indirect inhibition of RIP1 kinase. | ||
| M8570 | Apratastat | Others |
| Apratastat (TMI-005) is an orally active, potent and selective dual inhibitor of disintegrin metalloenzyme 17 (ADAM17/ TACE) and matrix metalloprotease (MMP). | ||
| M10482 | Forodesine hydrochloride | DNA/RNA Synthesis |
| BCX-1777 hydrochloride | ||
| Forodesine hydrochloride is a potent and orally active transition-state analog inhibitor of purine nucleoside phosphorylase, with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. | ||
| 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. | ||
| M10778 | Aldumastat | Others |
| GLPG1972 | ||
| Aldumastat (GLPG1972; S201086) is a potent, selective, orally active ADAMTS-5 (IC50=19 nM) inhibitor, whose selectivity is ADAMTS-4 (IC50=8 times 156 nM). Aldumastat has antimetabolic activity for osteoarthritis research. | ||
| M10943 | Atabecestat | BACE |
| JNJ-54861911 | ||
| Atabecestat (JNJ-54861911) is a potent brain-osmotic and has oral activity β-position amyloid precursor protein lyase 1 (BACE1 inhibitors that strongly reduce the expression of Aβ protein in cerebrospinal fluid. Atabecestat (JNJ-54861911) is tolerant and has sustained pharmacokinetic (PK) and pharmacodynamic (PD) profiles. Atabecestat (JNJ-54861911) has the potential to be used in the study of Alzheimer's disease. | ||
| 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. | ||
| 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. | ||
| M11321 | Angiopeptin TFA | Somatostatin Receptor |
| Angiopeptin TFA, a cyclic octapeptide analog of somatostatin, is an SST2 / SST5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA inhibits growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential to be used in the study of coronary atherosclerosis. | ||
| M13371 | Onametostat (JNJ-64619178) | PRMTs |
| Onametostat (JNJ-64619178) is a highly selective, orally active, pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (PRMT5-MEP-50, IC50=0.14 nM).Onametostat does not covalently bind to PRMT5, but has a long interaction time. It has good pharmacokinetic properties as well as safety profile. | ||
| 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. | ||
| M13670 | Domatinostat tosylate | HDAC |
| 4SC-202 | ||
| Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). | ||
| M13838 | Seclidemstat mesylate | Histone demethylase |
| SP-2577 mesylate | ||
| Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). | ||
| 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. | ||
| 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. | ||
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