YKL-5-124

Catalog No.S8863 Batch:S886301

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Technical Data

Formula

C28H33N7O3

Molecular Weight 515.61 CAS No. 1957203-01-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (193.94 mM)
* <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.)

Preparing Stock Solutions

Biological Activity

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.
Targets
CDK7 [1]
(Cell-free assay)
9.7 nM
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.

In vivo

YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor.

Protocol (from reference)

Animal Study:

[3]

  • Animal Models

    NSG female mice

  • Dosages

    2.5 mg/kg

  • Administration

    i.p.

Selleck's YKL-5-124 has been cited by 5 publications

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

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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.