YKL-5-124 | whatman (沃特曼)

YKL-5-124 纯度: 98.03%

YKL-5-124 是一种有效的、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。YKL-5-124 对 CDK7 的选择性比 CDK9 和 CDK2 高 100 倍以上，并且对 CDK12 和 CDK13 没有活性。YKL-5-124 诱导强烈的细胞周期停滞，并抑制 E2F 驱动的基因表达，并且对 RNA 聚合酶 II 磷酸化状态几乎没有影响。

YKL-5-124 Chemical Structure

CAS No. : 1957203-01-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2890	In-stock
5 mg	￥2550	In-stock
10 mg	￥4350	In-stock
25 mg	￥6960	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

YKL-5-124 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
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Anti-Blood Cancer Compound Library

生物活性

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].

IC₅₀ & Target^[1]

CDK7

53.5 nM (IC₅₀)

CDK7/Mat1/CycH

9.7 nM (IC₅₀)

CDK2

1300 nM (IC₅₀)

CDK9

3020 nM (IC₅₀)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	HAP1 cells
Concentration:	0 nM, 0.2 nM, 0.7 nM, 2 nM, 6.3 nM, 20 nM, 60 nM, 200 nM, 633.3 nM, 2000 nM
Incubation Time:	72 hours
Result:	Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells.

Western Blot Analysis^[1]

Cell Line:	HAP1 cells
Concentration:	0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
Incubation Time:	24 hours
Result:	Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion.

分子量

515.61

Formula

C₂₈H₃₃N₇O₃

CAS 号

1957203-01-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (193.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9395 mL	9.6973 mL	19.3945 mL
5 mM	0.3879 mL	1.9395 mL	3.8789 mL
10 mM	0.1939 mL	0.9697 mL	1.9395 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (4.03 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.03 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[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.

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