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SML2555

BIO-0919278 racemate

≥98% (HPLC)

Synonym(s):

BIO-0702697 racemate, BIO0702697 racemate, BIO0919278 racemate, Compound 702697 racemate, Compound 919278 racemate, N-(1H-Benzo[d]imidazol-2-yl)-2-(1-oxoisoindolin-2-yl)propenamide, N-1H-Benzimidazol-2-yl-1,3-dihydro-a-methyl-1-oxo-2H-isoindole-2-acetamide

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About This Item

Empirical Formula (Hill Notation):
C18H16N4O2
CAS Number:
Molecular Weight:
320.35
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

[nH]1c2c([nH][c]1=NC(=O)C(N3Cc4c(cccc4)C3=O)C)cccc2

InChI key

PWSSISUOJZBZFT-UHFFFAOYSA-N

Biochem/physiol Actions

BIO-0919278 is a highly selective cyclin-dependent kinase CDK12 inhibitor (Kd = 5.6 μM) with little or no potency against CDK1-7, CDK9, CDK14, CDK16-18 or 344 other kinases (<35% inhibition at 1 μM). BIO-0919278 reduces CDK12-mediated Pol II CTD Ser2 phosphorylation (by 57% at 1 μM; U-2 OS cells) without affecting CDK12-independent Pol II CTD Ser5 phosphorylation, and selectively targets noncanonical NF-κB activation (4-hr 20 ng/mLTWEAK-induced p52 nuclear translocation/NIK mRNA production IC50 = 167/320 nM; U-2 OS cells) without affecting canonical NF-κB activation (TNF-α-stimulated p65 (RelA) nuclear translocation IC50 >30 μM).
Highly selective CDK12 inhibitor that disrupts noncanonical, but not canonical, NF-κB activation.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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