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YKL-5-124 (TFA)

YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1].

Product Specifications

CAS Number

[2748220-93-9]

UNSPSC

12352005

Target

CDK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ykl-5-124-tfa.html

Purity

99.74

Solubility

DMSO : ≥ 100 mg/mL|H2O : 50 mg/mL (ultrasonic)

Smiles

CC1(C)N(C(N[C@@H](C2=CC=CC=C2)CN(C)C)=O)CC3=C1NN=C3NC(C4=CC=C(NC(C=C)=O)C=C4)=O.FC(F)(C(O)=O)F

Molecular Formula

C30H34F3N7O5

Molecular Weight

629.63

References & Citations

[1]Olson CM, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26 (6) :792-803.e10.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

CDK2; CDK7; CDK9

Citation 01

Adv Sci (Weinh) . 2024 Dec 10:e2413103.|Cell. 2025 Oct 30;188 (22) :6301-6316.e29.|bioRxiv. 2023 Apr 23.|bioRxiv. 2024 Dec 10:2024.12.09.627542.|bioRxiv. 2025 March 19.|Cell Death Discov. 2025 Mar 4;11 (1) :86.|Cell Discov. 2022 Oct 6;8 (1) :102.|EMBO J. 2025 Sep 8.|Int J Biol Sci. 2024 Aug 19;20 (11) :4513-4531.|Int J Mol Sci. 2023 Apr 10;24 (8) :7009.|iScience. 2024 May 16.|iScience. 2025 Nov 4;28 (12) :113925.|J Biomed Sci. 2022 Feb 14;29 (1) :13.|J Cancer Res Clin Oncol. 2023 Jul;149 (8) :5255-5263.|mBio. 2025 Dec 10;16 (12) :e0289825.|Res Sq. 2024 Jul 29.

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