YKL-5-124 [1957203-01-8]
Katalog-Nummer T22461-1mg
Size : 1mg
Marke : TargetMol
YKL-5-124
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YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13.
Cas No. 1957203-01-8
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Purity:99.36%
Appearance:Solid
Color:White
COA HNMR LCMS
Product Introduction
YKL-5-124 AI Summary
YKL-5-124 is a competitive irreversible inhibitor of CDK7/cyclin H/MNAT1, displaying an IC50 value of 53.0 nM in the presence of 1 mM ATP. It also inhibits CDK7 with an IC50 value of 9.7 nM, while showing limited inhibition of CDK2 (IC50 = 1300.0 nM) and CDK9 (IC50 > 3020.0 nM). The compound exhibits bioactivity in human HAP1 cells with an IC50 value of 53.5 nM based on a competitive pull-down assay. Additionally, it affects cell viability in different cell lines, demonstrating mixed inhibitory and stimulatory effects across various cell types, including HEK293T, U2OS, and human fibroblasts. Thermal Shift Assays indicate that YKL-5-124 stabilizes specific protein domains, with notable increases in melting temperature in segments M26-R383, M1-S360, E122-S403, S229-K512, and P449-E759, suggesting potential binding or stabilization effects within these regions..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13. |
| Targets & IC50 | CDK7-CyclinH-MAT1:9.7 nM, CDK2:1300 nM, CDK9:3020 nM, CDK7:53.5 nM |
| Molecular Weight | 515.61 |
| Formula | C28H33N7O3 |
| Cas No. | 1957203-01-8 |
| Smiles | CN(C)C[C@@H](NC(=O)N1Cc2c(NC(=O)c3ccc(NC(=O)C=C)cc3)n[nH]c2C1(C)C)c1ccccc1 |
| Relative Density. | 1.284 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (290.92 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (19.39 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (19.39 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||