product name TCS JNK 5a
Description: TCS JNK 5a, also known as JNK Inhibitor IX, is a highly selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. It is inactive at EGFR, ErbB2, VegFr2, Src, Tie-2, Alk5, c-Fms, CDK-2, GSK3β and PLK1 with pIC50 values of < 5.0. Exposure of human Jurkat T cells to SC-202671 targeting JNK2 and JNK3, caused apoptotic DNA fragmentation along with G2/M arrest, phosphorylation of Bcl-2, Mcl-1, and Bim, Δψm loss, and activation of Bak and caspase cascade.
References: Bioorg Med Chem Lett. 2007 Mar 1;17(5):1296-301.
332.42
Formula
C20H16N2OS
CAS No.
312917-14-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO:20 mg/mL (60.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
JNK Inhibitor IX
other peoduct :
| In Vitro |
In vitro activity: JNK inhibitor IX significantly reduces caspase-3 activity by the inhibition of JNK activity in human dermal fibroblasts. JNK inhibition by JNK inhibitor IX significantly increases apoptotic death in response to imatinib mesylate (IM) by preventing c-ABL complete de-phosphorylation at Ser residues. Kinase Assay: TCS JNK 5a is a selective JNK2 and JNK3 inhibitor. TCS JNK 5a exhibited selective against JNK1 and p38α with pIC50 values of 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38α, respectively. Also, TCS JNK 5a was inactive at EGFR, ErbB2, VegFr2, Src, Tie-2, Alk5, c-Fms, CDK-2, GSK3β and PLK1 with pIC50 values of < 5.0. Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2007 Mar 1;17(5):1296-301; Toxicol Lett. 2009 Aug 10;188(3):236-42. |
