JNK-IN-8|CAS 1410880-22-6|DC Chemicals

Cas No.:	1410880-22-6
Chemical Name:	(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide
Synonyms:	JNKIN 8
SMILES:	CC1=C(C=CC(=C1)NC(=O)C2=CC(=CC=C2)NC(=O)/C=C/CN(C)C)NC3=NC=CC(=N3)C4=CN=CC=C4
Formula:	C₂₉H₂₉N₇O₂
M.Wt:	507.59

Description:

JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

In Vitro:

JNK-IN-8 inhibits phosphorylation of c-Jun, a direct substrate of JNK kinase. JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 also exhibits exceptional selectivity based upon KinomeScan and enzymatic profiling. Cumulatively these combined profiling technologies demonstrate that both JNK-IN-8 and JNK-IN-12 are remarkably selective covalent JNK inhibitors and are appropriate for interrogating JNK-dependent biological phenomena[1]. JNK-IN-8, a selective pan-JNK inhibitor, is discovered to inhibit JNK kinase by broad-base kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeSca approach. JNK-IN-8 possess distinct regio-chemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic actemide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located towards the lip of the ATP-binding site[2].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7958	JNK-IN-8	JNK-IN-8 is a potent and irreversible JNK inhibitor that inhibits the phosphorylation of c-Jun.
DC2095	SP600125	SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM, respectively.
DC9694	IQ-1S	IQ-1S is a selective JNK3 inhibitor (IC50 values are 390, 360 and 87 nM for JNK1, 2 and 3 respectively).
DC7096	CC-401	CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.
DC7107	BI-78D3	BI-78D3 is a competitive c-Jun N-terminal kinase (JNK) inhibitor (IC50 = 280 nM) that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.