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Formula | C28H33N7O3 |
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Molecular Weight | 515.61 | CAS No. | 1957203-01-8 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (193.94 mM) | |
Ethanol | 100 mg/mL (193.94 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13. | ||
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Targets |
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In vitro | YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. |
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In vivo | YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor. |
Animal Study: |
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Redundant pathways for removal of defective RNA polymerase II complexes at a promoter-proximal pause checkpoint [ Mol Cell, 2024, S1097-2765(24)00835-9] | PubMed: 39504960 |
Preclinical modeling of leiomyosarcoma identifies susceptibility to transcriptional CDK inhibitors through antagonism of E2F-driven oncogenic gene expression [ Clin Cancer Res, 2022, clincanres.3523.2021] | PubMed: 35325095 |
CDK7/12/13 inhibition targets an oscillating leukemia stem cell network and synergizes with venetoclax in acute myeloid leukemia [ EMBO Mol Med, 2022, e14990] | PubMed: 35253392 |
TRF1 uses a noncanonical function of TFIIH to promote telomere replication [ Genes Dev, 2022, 36(17-18):956-969] | PubMed: 36229075 |
Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer [ Cell, 2021, 184(25):6119-6137.e26] | PubMed: 34890551 |
Transcriptional control of DNA repair networks by CDK7 regulates sensitivity to radiation in MYC-driven medulloblastoma [ Cell Rep, 2021, 35(4):109013] | PubMed: 33910002 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.