(E/Z)-THZ1 dihydrochloride | THZ1 Dihydrochloride;THZ1 2HCl | CDK

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(E/Z)-THZ1 dihydrochloride {[allProObj[0].p_purity_real_show]}

货号：A303658 同义名： THZ1 Dihydrochloride;THZ1 2HCl

THZ1 2HCl is a Cdk7 inhibitor (IC50s = 3.2-15.6 nM in vitro) that selectively targets a remote cysteine residue located outside of the classic kinase domain. THZ1 2HCl also targets Cdk12 kinase activity although at a higher concentration (IC50 = 250 nM).

(E/Z)-THZ1 dihydrochloride 化学结构
CAS号：2095433-94-4

(E/Z)-THZ1 dihydrochloride 3D分子结构
CAS号：2095433-94-4

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(E/Z)-THZ1 dihydrochloride 纯度/质量文件产品仅供科研

货号：A303658 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(E/Z)-THZ1 dihydrochloride 生物活性

靶点	CDK7 CDK7, IC50:3.2 nM
描述	CDK7, belonging to the CDK family, can form part of the TFIIH complex with Cyclin H/MAT1 and regulate RNA polymerase II transcription and DNA repair.^[2] THZ1 is a highly selective inhibitor of CDK7 with IC50 value of 3.2nM (measured by THZ1 enzymatic activity). Treatment with THZ1≥250nM for 4h can completely inhibit the phosphorylation of the established intracellular RNAPII CTD, the substrate of CDK7, at Ser 5 and Ser 7 in Jurkat cells, with concurrent loss of Ser 2 phosphorylation. THZ1 on concentration of 250nM can reduced RNAPII occupancy genome wide at both promoters and gene bodies in while Flavopiridol reduced RNAPII density only across gene bodies. THZ1 showed broad-based activity with half-maximum inhibitory concentration (IC50) values less than 200nM against 598 cell lines, which have a strong enrichment of common expression of (proto-) oncogenic transcription factors involved in RNAPII-driven transcriptional regulation. Intravenous treatment of THZ1 10mg/kg once daily or twice days for 29 days exhibited efficacy in a human T-ALL cell-line KOPTK1 xenografted mouse model^[1].
作用机制	THZ1 is a covalent CDK7 inhibitor which can target ATP-binding pocket of CDK7.^[1]

(E/Z)-THZ1 dihydrochloride 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
Jurkat cells		Cytotoxicity assay	72 h	Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay, IC50=0.05 μM	26115571

(E/Z)-THZ1 dihydrochloride 动物研究

Dose	Mice: 10 mg/kg i.p.^[3] i.v.^[4]
Administration	i.p., i.v.

(E/Z)-THZ1 dihydrochloride 参考文献

[1]Kwiatkowski N, Zhang T, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.

[2]Roskoski R Jr, et al. Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs. Pharmacol Res. 2016 May;107:249-275.

[3]Wang Y, Zhang T, et al. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015;163(1):174-86.

[4]Chipumuro E, Marco E, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014;159(5):1126-1139.

(E/Z)-THZ1 dihydrochloride 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.56mL

0.31mL

0.16mL

7.83mL

1.56mL

0.78mL

15.65mL

3.13mL

1.56mL

(E/Z)-THZ1 dihydrochloride 技术信息

CAS号	2095433-94-4
分子式	C₃₁H₃₀Cl₃N₇O₂
分子量	638.975

别名	THZ1 Dihydrochloride;THZ1 2HCl
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

动物实验配方

5% DMSO+45% PEG 300+water 4 mg/mL

(E/Z)-THZ1 dihydrochloride {[allProObj[0].p_purity_real_show]}

(E/Z)-THZ1 dihydrochloride 纯度/质量文件产品仅供科研

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全球学术期刊中引用的产品

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(E/Z)-THZ1 dihydrochloride 生物活性

(E/Z)-THZ1 dihydrochloride 细胞研究

(E/Z)-THZ1 dihydrochloride 动物研究

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(E/Z)-THZ1 dihydrochloride 实验方案

(E/Z)-THZ1 dihydrochloride 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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