YKL-5-124

Name: YKL-5-124
Brand: TargetMol
SKU: T22461
Price: 787 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.36%

货号 T22461Cas号 1957203-01-8

YKL-5-124 是选择性不可逆CDK7共价抑制剂，对CDK7和CDK7/Mat1/CycH 的IC50分别为 53.5 nM 和 9.7 nM。它诱导强烈的细胞周期停滞，并抑制 E2F 驱动的基因表达。它对 CDK7 的生化和细胞选择性优于 CDK12/13。它对CDK7的选择性比 CDK9 和 CDK2 高 100 倍以上。

YKL-5-124

一键复制产品信息

很棒

纯度: 99.36%

货号 T22461Cas号 1957203-01-8

规格	价格	库存
1 mg	¥ 787	现货
5 mg	¥ 1,790	现货
10 mg	¥ 2,880	现货
25 mg	¥ 4,580	现货
50 mg	¥ 6,430	现货
100 mg	¥ 8,680	现货
1 mL x 10 mM (in DMSO)	¥ 1,980	现货

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纯度: 99.36%

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COA HNMR LCMS 产品操作手册

产品介绍

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

生物活性

产品描述	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.
靶点活性	CDK9:3020 nM, CDK2:1300 nM, CDK7:53.5 nM, CDK7-CyclinH-MAT1:9.7 nM

化学信息

分子量	515.61
分子式	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
密度	1.284 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

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.

溶解度信息

DMSO: 220 mg/mL (426.68 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.7 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9395 mL	9.6973 mL	19.3945 mL	96.9725 mL
5 mM	0.3879 mL	1.9395 mL	3.8789 mL	19.3945 mL
10 mM	0.1939 mL	0.9697 mL	1.9395 mL	9.6973 mL
20 mM	0.0970 mL	0.4849 mL	0.9697 mL	4.8486 mL
50 mM	0.0388 mL	0.1939 mL	0.3879 mL	1.9395 mL
100 mM	0.0194 mL	0.0970 mL	0.1939 mL	0.9697 mL