YKL-5-124

Product Name: YKL-5-124
CAS No.: 1957203-01-8
Chemical Name: YKL-5-124
Synonyms: YKL-5-124;(S)-3-(4-Acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[[4-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]-;T-loop,phosphorylation,inhibit,arrest,CDK7,Inhibitor,CDK,YKL5124,YKL 5 124,CDK7/Mat1/CycH,Cyclin dependent kinase,cell-cycle,transcription,Pol-II,irreversible,covalent
CBNumber: CB85867444
Molecular Formula: C28H33N7O3
Formula Weight: 515.61
MOL File: 1957203-01-8.mol

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YKL-5-124 Property

Boiling point:: 706.1±60.0 °C(Predicted)
Density: 1.284±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 250 mg/mL (484.86 mM; Need ultrasonic)
pka: 12.78±0.40(Predicted)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3039
Product name: YKL-5-124
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $113
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML3039
Product name: YKL-5-124
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $568
Updated: 2024/03/01

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YKL-5-124 Chemical Properties,Usage,Production

Biological Activity

YKL-5-124 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 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1]. YKL-5-124 (0-2000 nM; 72 hours; HAP1 cells) treatment causes a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells[1].YKL-5-124 (0-2000 nM; 24 hours; HAP1 WT cells) treatment inhibits CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion[1].Treatment of cells with YKL-5-124 as a competitor at a concentration of about 30 nM blocks pull-down of CDK7-cyclin H but has no effect on the pull-down of cyclin K-CDK12/13 in HAP1 cells. Treatment with 100 nM YKL-5-124 reduces CDK7-cyclin H binding to bioTHZ1 by >50% at 30 min[1].

storage

Store at -20°C

References

[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.

YKL-5-124 Preparation Products And Raw materials

Raw materials

Preparation Products

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YKL-5-124 Suppliers

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1957203-01-8, YKL-5-124Related Search:

yk11 YK-4-279 2-(4-HYDROXY-3-METHOXYPHENYL)BENZOTHIAZOLE YKL 06-061 YL 0919

YKL-5-124

Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[[4-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]-

(S)-3-(4-Acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide

T-loop,phosphorylation,inhibit,arrest,CDK7,Inhibitor,CDK,YKL5124,YKL 5 124,CDK7/Mat1/CycH,Cyclin dependent kinase,cell-cycle,transcription,Pol-II,irreversible,covalent

1957203-01-8

C28H33N7O3