About 32 results found for searched term "STAT3-IN-3" (0.091 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M14149 | STAT3-IN-3 | STAT |
| STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. | ||
| M49681 | STAT3-IN-13 | STAT |
| STAT3-IN-13 is a potent STAT3 inhibitor. | ||
| M49685 | STAT3-IN-23 | STAT |
| STAT3-IN-23 (PY*LKTK) is a potent STAT3 inhibitor. | ||
| M9217 | Givinostat | HDAC |
| ITF2357 | ||
| Givinostat (ITF-2357) is an HDAC inhibitor with IC50s of 198 and 157 nM for HDAC1 and HDAC3, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| M3001 | SC144 | IL Receptor/Related |
| SC144 is the first oral active GP130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, eliminates Stat3 phosphorylation and nuclear translocation, and further inhibits downstream target gene expression. SC144 inhibited signal transduction induced by GP130 ligand. SC144 induces apoptosis of human ovarian cancer cells. | ||
| 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). | ||
| M11542 | Ochromycinone | STAT |
| (Rac)-STA-21；STA 21 | ||
| Ochromycinone ((RAC-STA-21) is a natural antibiotic and a selective inhibitor of STAT3. Ochromycinone can inhibit STAT3 DNA binding activity and STAT3 dimerization. Ochromycinone has anticancer and antibacterial activities. | ||
| M4288 | Atractylenolide I | TLR |
| Atractylenolide I is a sesquiterpene obtained from the roots of Atractylenolide. Atractylenolide I has neuroprotective, anti-allergic, anti-inflammatory and anticancer activities. Atractylenolide I is an antagonist of TLR4 and can also reduce the phosphorylation of JAK2 and STAT3 in A375 cells. | ||
| M4433 | Alantolactone | STAT |
| (+)-Alantolactone; Alant camphor; Elecampane camphor; Eupatal; Inula camphor | ||
| Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone (helenin, helenine, Eupatal) could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction. | ||
| 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. | ||
| M5807 | Napabucasin (BBI608) | STAT |
| BBI608; BB608 | ||
| Napabucasin (BBI608) is a first-in-class, orally active inhibitor of Stat3 that blocks stem cell activity in cancer cells by targeting the signal transducer and activator of transcription 3 pathway. Napabucasin inhibits cell proliferation of U87MG tumor xenografts in mice. | ||
| 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). | ||
| M7273 | SC 144 hydrochloride | IL Receptor/Related |
| SC144 hydrochloride is the first oral active GP130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, inducing phosphorylation (S782) and deglycosylation of GP130, eliminating Stat3 phosphorylation and nuclear translocation, and further inhibiting the expression of downstream target genes. SC144 hydrochloride inhibited signal transduction induced by GP130 ligand. SC144 hydrochloride induces apoptosis of human ovarian cancer cells. | ||
| 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. | ||
| M7754 | 5, 15-DPP | STAT |
| 5, 15-DPP is a selective STAT3 inhibitor and a selective STAT3-SH2 antagonist. | ||
| M7811 | FLLL31 | STAT |
| FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. | ||
| M8983 | Compstatin | Complement System |
| ICVVQDWGHHRCT | ||
| Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. Compstatin exhibits exclusive specificity for primate C3s and does not bind either to C3s from lower mammalian species or to two structural homologs of C3, human C4 and C5. | ||
| M9386 | Verubecestat (MK-8931) | BACE |
| MK-8931 | ||
| Verubecestat (MK-8931) is an orally active, high-affinity (beta-secretase 1) BACE1 and BACE2 inhibitor, with Ki values of 2.2 nM and 0.38 nM, respectively. | ||
| M10514 | Verdiperstat (AZD3241) | Others |
| AZD3241; BHV-3241; CAS#890655-80-8 | ||
| Verdiperstat (AZD-3241) is a selective and irreversible inhibitor of myeloperoxidase (MPO) with an IC50 of 630 nM. | ||
| M10696 | Protosappanin A | JAK |
| 原苏木素A; PTA | ||
| Protosappanin A (PTA), an immune agent, is a major biphenyl compound isolated from Caesalpinia sappan L that inhibits the JAK2/STAT3-dependent inflammatory pathway by down-regulating the phosphorylation of JAK2 and STAT3. | ||
| M14075 | Compstatin TFA | Complement System |
| Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. | ||
| 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. | ||
| M14473 | Prinomastat | MMP |
| AG3340; KB-R9896 | ||
| Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. | ||
| 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. | ||
| M21406 | SI-109 | STAT |
| SI-109 is a potent STAT3 SH2 domain structural domain inhibitor (Ki=9 nM) with antitumor activity. si-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). si-109 and the CRBN analogue lenalidomide ligand were used to design the PROTAC STAT3 degradation agent SD- 36. | ||
| M21510 | Telaglenastat hydrochloride | Others |
| CB-839 hydrochloride | ||
| Telaglenastat (CB-839) hydrochloride is a pioneering (first-in-class), selective, reversible, orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride has IC50 values of 23 nM and 28 nM for endogenous glutaminase in the kidney and brain of mice, respectively. Telaglenastat hydrochloride also induces autophagy and has strong antitumor activity. | ||
| M21677 | Recombinant Human Follistatin 288 (Mammalian, C-6His) | Recombinant Proteins |
| FST; follistatin isoform FST317 | ||
| Follistatin 288 is a secreted glycoprotein that was first identified as a follicle-stimulating hormone inhibiting substance in ovarian follicular fluid . Human follistatin 288 cDNA encodes a 317 amino acid (aa) protein with a 29 aa signal sequence, and a 288 aa mature region. Recombinant Human Follistatin/FST is produced by Mammalian expression system and the target gene encoding Gly30-Asn317 is expressed with a 6His tag at the C-terminus. | ||
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