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TCS 21311JAK3 inhibitor

TCS 21311

Catalog No. A4516
Size Price Stock Qty
10mg $252.00 In stock
50mg $1,062.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TCS 21311

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Chemical Properties

Cas No. 1260181-14-3 SDF Download SDF
Chemical Name 3-[5-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
Canonical SMILES CC(C)(C(=O)N1CCN(CC1)C2=CC(=C(C=C2)C(F)(F)F)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54)O
Formula C27H25F3N4O4 M.Wt 526.51
Solubility Soluble in DMSO > 10 mM Storage Desiccate at RT
General tips N/A
Shipping Condition N/A

Background

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].

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.