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Compound 919278

Chemical Structure : Compound 919278

CAS No.: 2189366-77-4

Compound 919278 (CDK12 inhibitor Compound 919278)

Catalog No.: PC-35532Not For Human Use, Lab Use Only.

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK.
Compound 919278 does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA).
Compound 919278 prevents the accumulation of NIK, selectively inhibits the noncanonical NF-kB pathway.
Compound 919278 prevents the LTβR- and FN14-dependent expression of MAP3K14 (which encodes NIK) as well as NIK accumulation by reducing phosphorylation of the carboxyl-terminal domain of RNA polymerase II.
Compound 919278 reduces the binding of both CDK12 and its associated protein CCNK with IC50 of 30-60 nM, inhibits CDK12 cellular activity and reduces the phosphorylation of Ser2 on the RNA Pol II CTD.
Compound 919278 phenocopies the effect of CDK12 knockdown on DEGs.

Physicochemical Properties

M.Wt 320.352
Formula C18H16N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(1H-benzo[d]imidazol-2-yl)-2-(1-oxoisoindolin-2-yl)propanamide

References

1. Henry KL, et al. Sci Signal. 2018 Jul 31;11(541). pii: eaam8216.

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