| Identification | Back Directory | [Name]
TCS 21311 | [CAS]
1260181-14-3 | [Synonyms]
TCS 21311
NIBR-3049
TCS21311; TCS-21311
JAK3/GSK-3β/PKCα Inhibitor - CAS 1260181-14-3 - Calbiochem
3-{5-[4-(2-hydroxy-2-methylpropionyl)piperazin-1-yl]-2-trifluoromethylphenyl}-4-(1H-indol-3-yl)pyrrole-2,5-dione
3-[5-[4-(2-Hydroxy-2-Methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoroMethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-[5-[4-(2-hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)- | [Molecular Formula]
C27H25F3N4O4 | [MOL File]
1260181-14-3.mol | [Molecular Weight]
526.51 |
| Chemical Properties | Back Directory | [Boiling point ]
793.0±60.0 °C(Predicted) | [density ]
1.436±0.06 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
<52.65mg/ml in DMSO | [form ]
Yellow solid | [pka]
7.91±0.60(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
A potent JAK3 inhibitor; selective for JAK3 over JAK1, JAK2 and TYK2. It also inhibits GSK-3β, PKCα and PKCθ. | [Biological Activity]
tcs 21311 is a potent and selective jak3 inhibitor with the ic50 values of 8 nm. tcs 21311 shows high selectivity for jak3 over jak1, jak2 and tyk2. the ic50 values are 1017, 2550 and 8055 nm respectively. tcs 21311 exihibits inhibitory effect on gsk-3β, pkcα and pkcθ with the ic50 values of 3, 13 and 68 nm, respectively [1].janus kinases (jak) belong to a small family of cytoplasmic protein tyrosine kinases including jak1, jak2, tyk2, and jak3, which play important roles in initiating the cytokine-triggered signaling events by activators of transcription (stat) proteins via tyrosine phosphorylation [2]. due to its association with relevant cytokine signaling pathways, jak3 serves as an important target for therapeutic intervention in the treatment of inflammatory diseases, autoimmune disorders and organ transplant rejection [2]. | [IC 50]
JAK3: 8 nM (IC50); JAK2: 2.55 μM (IC50); JAK1: 1.017 μM (IC50); PKCα: 13 nM (IC50); PKCθ: 68 nM (IC50); GSK-3β: 3 nM (IC50) | [storage]
Desiccate at RT | [References]
[1] thoma g, nuninger f, falchetto r, et al. identification of a potent janus kinase 3 inhibitor with high selectivity within the janus kinase family[j]. journal of medicinal chemistry, 2010, 54(1): 284-288.
[2] clark m p, george k m, bookland r g, et al. development of new pyrrolopyrimidine-based inhibitors of janus kinase 3 (jak3)[j]. bioorganic & medicinal chemistry letters, 2007, 17(5): 1250-1253. |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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