YKL-5-124
Modify Date: 2024-01-04 11:55:13
YKL-5-124 structure
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Common Name | YKL-5-124 | ||
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| CAS Number | 1957203-01-8 | Molecular Weight | 515.618 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H33N7O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of YKL-5-124YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM; displays biochemical and cellular selectivity for CDK7 over structurally related kinases CDK12/13, and no significant activity against CDK2 and CDK9 (IC50>1 uM); targets and forms a covalent bond with CDK7- cysteine 312 (C312); inhibition of CDK7 by YKL-5-124 elicits a transcriptional signature distinct from that of THZ1, shows no discernible effect on RNA Pol II CTD phosphorylation; recapitulate THZ1-mediated effects on gene expression and CTD phosphorylation when combined with CDK12/13 inhibitor THZ531. |
| Name | YKL-5-124 |
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| Description | YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM; displays biochemical and cellular selectivity for CDK7 over structurally related kinases CDK12/13, and no significant activity against CDK2 and CDK9 (IC50>1 uM); targets and forms a covalent bond with CDK7- cysteine 312 (C312); inhibition of CDK7 by YKL-5-124 elicits a transcriptional signature distinct from that of THZ1, shows no discernible effect on RNA Pol II CTD phosphorylation; recapitulate THZ1-mediated effects on gene expression and CTD phosphorylation when combined with CDK12/13 inhibitor THZ531. |
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| References | References 1. Olson CM, et al. Cell Chem Biol. 2019 Mar 6. pii: S2451-9456(19)30067-4. View Related Products by Target Cyclin-dependent Kinase (CDK) |
| Molecular Formula | C28H33N7O3 |
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| Molecular Weight | 515.618 |
| Hazard Codes | Xi |
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