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  3. HIT219500671
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HIT219500671
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HIT219500671
  • HIT ID:HIT219500671
  • Cas No:2088715-91-5
  • 常用名:MFH290
  • IUPAC:N-{4-[(3R)-3-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)amino]piperidine-1-carbonyl]phenyl}prop-2-enamide
    IUPAC:N-{4-[(3R)-3-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)amino]piperidine-1-carbonyl]phenyl}prop-2-enamide
  • InChI key:COGUZYALRYMQTD-LJQANCHMSA-N
  • 分子式:C26H31N5O3S2
  • 分子量:525.69
  • 氢键供体数 (HBD):
  • 氢键受体数 (HBA):
  • LogP:
  • SMILES:CC(C)(C)c1cnc(CSc2cnc(N[C@@H]3CCCN(C3)C(=O)c3ccc(NC(=O)C=C)cc3)s2)o1
    SMILES:CC(C)(C)c1cnc(CSc2cnc(N[C@@H]3CCCN(C3)C(=O)c3ccc(NC(=O)C=C)cc3)s2)o1
  • MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.
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  • 供应商
    TargetMolSC
    规格
    货期
    6-8周
    纯度
    -
    ¥ 11,700.00
    1

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