About 28 results found for searched term "STAT6-IN-3" (0.127 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M42114 | STAT6-IN-3 | STAT |
| STAT6-IN-3 is a STAT6 inhibitor (IC50= 44 nM). | ||
| M2147 | Ilomastat | MMP |
| GM6001; Galardin | ||
| Ilomastat (GM6001; Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor with Ki values of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM and 0.36 nM for MMPs -1, -2, -3, -7, -8, -9, -12, -14 and -26, respectively. Ilomastat (GM6001; Galardin) reduces infarct volume following middle cerebral artery occlusion in an ischemic mouse model. | ||
| 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. | ||
| M2883 | Nifuroxazide | STAT |
| Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells. | ||
| M5233 | Osilodrostat | Mineralocorticoid Receptor |
| LCI699 | ||
| Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. | ||
| 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. | ||
| M6136 | Epacadostat | IDO |
| INCB024360 | ||
| Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). | ||
| M6287 | GLPG1690 | PDE |
| Ziritaxestat | ||
| Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with IC50 of 131 nM and Ki of 15 nM. | ||
| M6700 | Eeyarestatin I | Others |
| Eeyarestatin-I | ||
| Eeyarestatin I is a potent endoplasmic reticulum-associated protein degradation (ERAD) and translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. | ||
| M14297 | Fidarestat | Others |
| SNK 860 | ||
| Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease. | ||
| M15047 | Recombinant Mouse OSM (HEK 293) | Cytokines and Growth Factors |
| OncoM; oncostatin M | ||
| Protein Construction：OSM (Ala24-Arg206) Oncostatin M (OSM) is a multifunctional cytokine belonging to the interleukin-6 (IL-6) subfamily, which also includes IL-11, leukemia suppressor (LIF), ciliary nerve promoter, cardiac trophic factor-1 and novel nerve promoter factor-1. Protein structure: OSM (ALA24-ARG206), Accession # : P53347. | ||
| M17579 | Brevilin A | Sesquiterpenoids |
| Brevilin A is an orally active STAT3/JAK inhibitor, with IC50 of 10.6 μM against STAT3. | ||
| M19040 | Bruceantinol | STAT |
| Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50=2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. | ||
| 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. | ||
| M21159 | SD-36 | PROTAC |
| SD-36 is a potent STAT3 PROTAC degradation agent (Kd=~50 nM) with a high selectivity compared to other STAT members. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. | ||
| M21381 | AS1810722 | STAT |
| AS1810722 is an orally effective STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows good CYP3A4 inhibition and is a thickened bicyclic pyrimidine derivative with potential for use in allergic disease studies, such as asthma and atopic diseases. | ||
| M27774 | Crebinostat | HDAC |
| Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. | ||
| M28169 | Osilodrostat phosphate | Mineralocorticoid Receptor |
| LCI699 phosphate | ||
| Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. | ||
| M28184 | Debio 0617B | STAT |
| Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34+ stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors. | ||
| 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. | ||
| M28738 | (S)-PM-43I | STAT |
| (S)-PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. (S)-PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research. | ||
| M29911 | BRD9876 | Kinesin |
| BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research. | ||
| M30035 | Spliceostatin A | Others |
| Spliceostatin A, the FR901464 methylated derivative, is a potent anti-tumor agent. Spliceostatin A inhibits splicing and promotes pre-mRNA accumulation by binding SF3B1. SF3B1 is a subcomplex of U2 small nuclear ribonucleoprotein in the spliceosome. Spliceostatin A induces Apoptosis in chronic lymphocytic leukemia (CLL) cells. | ||
| M30649 | C188 | STAT |
| CPD188 | ||
| C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM). | ||
| M39838 | Zederone | mTOR |
| Zederone, a germacrane-type sesquiterpene, has potently cytotoxic against human white blood cancer cells and human prostate cancer cells. Zederone significantly inhibits the proliferation and downregulates the protein expressions of mTOR, and phosphorylated p70 S6 kinase (p-p70s6K) in SKOV3 cells. | ||
| M40707 | Icotrokinra | IL Receptor/Related |
| JNJ-2113; JNJ-77242113; PN-235 | ||
| Icotrokinra (JNJ-77242113, JNJ-2113) is a novel, orally active IL-23R peptide antagonist for studies related to plaque psoriasis. Icotrokinra exhibits high affinity with human IL-23 receptor hIL-23R with a Kd of 7.1 pM. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in PMBCs (IC50=5.6 pM), and inhibits L-23-induced generation of IFNγ and IL-17A in picomolar levels. | ||
| M41940 | PRL 3195 | Somatostatin Receptor |
| PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively). | ||
| M49680 | STAT3-IN-12 | STAT |
| STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. | ||
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