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About This Item
Empirical Formula (Hill Notation):
C18H16N4O2
CAS Number:
Molecular Weight:
320.35
UNSPSC Code:
12352200
NACRES:
NA.77
InChI key
PWSSISUOJZBZFT-UHFFFAOYSA-N
SMILES string
[nH]1c2c([nH][c]1=NC(=O)C(N3Cc4c(cccc4)C3=O)C)cccc2
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Related Categories
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
Regulatory Information
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