YKL 5-124

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Description: Potent and selective CDK7 inhibitor; induces cell cycle arrest
Chemical Name: N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[[4-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
Purity: ≥95% (HPLC)

Biological Activity for YKL 5-124

YKL-5-124 is a potent and selective CDK7/Mat1/CycH and cyclin dependent kinase (CDK7) inhibitor (IC50 values = 9.7 nM and 53.5 nM, respectively). YKL-5-124 shows 100-fold selectivity over CDK9 and CDK2. YKL-5-124 induces cell cycle arrest at the G1/S transition, inhibits E2F-driven gene expression and inhibits CDK1 and CDK3 T-loop phosphorylation.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data for YKL 5-124

M. Wt 515.62
Formula C28H33N7O3
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 1957203-01-8
PubChem ID 121443990
Smiles CN(C[C@H](C1=CC=CC=C1)NC(N2CC3=C(C2(C)C)NN=C3NC(C4=CC=C(C=C4)NC(C=C)=O)=O)=O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for YKL 5-124

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 10.31 20
ethanol 10.31 20

Preparing Stock Solutions for YKL 5-124

The following data is based on the product molecular weight 515.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.7 mL 48.49 mL 96.97 mL
1 mM 1.94 mL 9.7 mL 19.39 mL
2 mM 0.97 mL 4.85 mL 9.7 mL
10 mM 0.19 mL 0.97 mL 1.94 mL

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References for YKL 5-124

References are publications that support the biological activity of the product.

Olson et al (2019) Development of a selective CDK7 covalent inhibitor reveals predominant cell-cycle phenotype. Cell Chem.Biol. 26 792 PMID: 30905681

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