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CDK12-IN-E9

CAS No. : 2020052-55-3

產(chǎn)品活性：CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC₅₀> 1 μM.

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點：CDK

In Vitro: CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1^R NB and lung cancer cells, with IC₅₀ values ranging from 8 to 40 nM.
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1^r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression.
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1^r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9.

相關(guān)產(chǎn)品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  SY-5609  |  CLK1/2-IN-1  |  SB-218078  |  Toyocamycin  |  (S)-LY3177833 hydrate  |  Dinaciclib  |  EGFR/HER2/CDK9-IN-2  |  CDK8-IN-11  |  SNS-032  |  M2N12  |  Palbociclib-d₈  |  EGFR/CDK2-IN-1  |  BSJ-04-132  |  (E/Z)-Zotiraciclib  |  CCT-251921  |  BS-181  |  Ribociclib-d₈  |  CDK9-IN-9  |  Flavopiridol  |  SRI-29329  |  dCeMM4  |  GSK 3 Inhibitor IX  |  CDK9-IN-7  |  BSJ-03-204  |  Amantadine-d₆  |  K00546  |  Abemaciclib metabolite M18 hydrochloride  |  Ribociclib-d₆  |  Lacto-N-fucopentaose I  |  CDK2/4/6-IN-2

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