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

(E/Z)-THZ1 2HCl {[allProObj[0].p_purity_real_show]}

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

(E/Z)-THZ1 dihydrochloride是一种 Cdk7 抑制剂 (IC50 介于 3.2-15.6 nM)，选择性靶向经典激酶域之外的远端半胱氨酸残基，对 Cdk12 的激酶活性抑制作用较高 (IC50 = 250 nM)。

(E/Z)-THZ1 2HCl 化学结构
CAS号：2095433-94-4

(E/Z)-THZ1 2HCl 3D分子结构
CAS号：2095433-94-4

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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 HCl	++++ 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(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
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 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ 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				99%
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			98%
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 2HCl 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 2HCl 细胞实验

Cell Line NSCLC cells PancVH1 cells HPNE cells Kasumi-1 cells U266 cells HeLa cells NPC cells H4 cells U87 cells U251 cells	Concentration	Treated Time	Description	References
NSCLC cells	50 nM	48 hours	THZ1 promotes apoptosis and suppresses NSCLC growth	J Hematol Oncol. 2020 Jul 20;13(1):99.
PancVH1 cells	500 nM	24 hours	Induces caspase-8 dependent apoptosis	Cancer Res. 2022 Sep 16;82(18):3375-3393.
HPNE cells	500 nM	24 hours	No significant apoptosis observed	Cancer Res. 2022 Sep 16;82(18):3375-3393.
Kasumi-1 cells	400 nM	1 hour	THZ1 treatment affects RNA polymerase dynamics and induces rapid apoptosis.	Nucleic Acids Res. 2019 May 7;47(8):3921-3936.
U266 cells	50-400 nM	24 hours	THZ1 significantly reduced phosphorylation of RNA Pol II, indicating inhibition of transcription	Clin Cancer Res. 2019 Oct 15;25(20):6195-6205.
HeLa cells	0.03 - 0.3 µM	30 minutes	To investigate the effects of THZ1 on Pol II phosphorylation, co-transcriptional capping, promoter proximal pausing, and productive elongation. THZ1 does not affect initiation but blocks essentially all Pol II large subunit C-terminal domain (CTD) phosphorylation.	Mol Cell. 2015 Aug 20;59(4):576-87.
NPC cells	200 nM	6 hours	To assess the dose response and anti-cancer effects of THZ1, showing significant inhibition of cell growth and induction of apoptosis.	Cancer Res. 2017 Dec 1;77(23):6614-6626.
H4 cells	150 nM (IC50)	72 hours	To evaluate the effect of THZ1 on the viability of H4 cells, results showed that THZ1 significantly inhibited the viability of H4 cells.	Neuro Oncol. 2024 Jan 5;26(1):70-84.
U87 cells	38.29 nM (IC50)	72 hours	To evaluate the effect of THZ1 on the viability of U87 cells, results showed that THZ1 significantly inhibited the viability of U87 cells.	Neuro Oncol. 2024 Jan 5;26(1):70-84.
U251 cells	120.3 nM (IC50)	72 hours	To evaluate the effect of THZ1 on the viability of U251 cells, results showed that THZ1 significantly inhibited the viability of U251 cells.	Neuro Oncol. 2024 Jan 5;26(1):70-84.

Cell Line

Concentration

Treated Time

Description

References

NSCLC cells

50 nM

48 hours

THZ1 promotes apoptosis and suppresses NSCLC growth

J Hematol Oncol. 2020 Jul 20;13(1):99.

PancVH1 cells

500 nM

24 hours

Induces caspase-8 dependent apoptosis

Cancer Res. 2022 Sep 16;82(18):3375-3393.

HPNE cells

500 nM

24 hours

No significant apoptosis observed

Cancer Res. 2022 Sep 16;82(18):3375-3393.

Kasumi-1 cells

400 nM

1 hour

THZ1 treatment affects RNA polymerase dynamics and induces rapid apoptosis.

Nucleic Acids Res. 2019 May 7;47(8):3921-3936.

U266 cells

50-400 nM

24 hours

THZ1 significantly reduced phosphorylation of RNA Pol II, indicating inhibition of transcription

Clin Cancer Res. 2019 Oct 15;25(20):6195-6205.

HeLa cells

0.03 - 0.3 µM

30 minutes

To investigate the effects of THZ1 on Pol II phosphorylation, co-transcriptional capping, promoter proximal pausing, and productive elongation. THZ1 does not affect initiation but blocks essentially all Pol II large subunit C-terminal domain (CTD) phosphorylation.

Mol Cell. 2015 Aug 20;59(4):576-87.

NPC cells

200 nM

6 hours

To assess the dose response and anti-cancer effects of THZ1, showing significant inhibition of cell growth and induction of apoptosis.

Cancer Res. 2017 Dec 1;77(23):6614-6626.

H4 cells

150 nM (IC50)

72 hours

To evaluate the effect of THZ1 on the viability of H4 cells, results showed that THZ1 significantly inhibited the viability of H4 cells.

Neuro Oncol. 2024 Jan 5;26(1):70-84.

U87 cells

38.29 nM (IC50)

72 hours

To evaluate the effect of THZ1 on the viability of U87 cells, results showed that THZ1 significantly inhibited the viability of U87 cells.

Neuro Oncol. 2024 Jan 5;26(1):70-84.

U251 cells

120.3 nM (IC50)

72 hours

To evaluate the effect of THZ1 on the viability of U251 cells, results showed that THZ1 significantly inhibited the viability of U251 cells.

Neuro Oncol. 2024 Jan 5;26(1):70-84.

(E/Z)-THZ1 2HCl 动物实验

Species Mice Mice Mice NOD/SCID-γ mice	Animal Model Lewis lung carcinoma model Xenograft model U251-luc orthotopic xenograft model Systemic U266 xenograft model	Administration	Dosage	Frequency	Description	References
Mice	Lewis lung carcinoma model	Intraperitoneal injection	10 mg/kg	Twice daily	Enhanced anti-PD-1 therapy efficacy	J Hematol Oncol. 2020 Jul 20;13(1):99.
Mice	Xenograft model	Intraperitoneal injection	10 mg/kg	Twice daily for 4 weeks	To evaluate tumor growth inhibition and assess the tumor-suppressive function of THZ1.	Cancer Res. 2017 Dec 1;77(23):6614-6626.
Mice	U251-luc orthotopic xenograft model	IntratumOral injection	10 mg/kg	Continuous infusion for 4 weeks	To evaluate the effect of SNS032 on the growth of orthotopic U251-luc tumors, results showed that SNS032 significantly inhibited tumor growth and extended the survival of mice.	Neuro Oncol. 2024 Jan 5;26(1):70-84.
NOD/SCID-γ mice	Systemic U266 xenograft model	Intraperitoneal injection	10 mg/kg	Once daily, 5 days/week for 4 weeks	THZ1 significantly reduced tumor burden and prolonged survival with minimal toxicity	Clin Cancer Res. 2019 Oct 15;25(20):6195-6205.

Species

Mice Mice Mice NOD/SCID-γ mice

Animal Model

Lewis lung carcinoma model Xenograft model U251-luc orthotopic xenograft model Systemic U266 xenograft model

Administration

Dosage

Frequency

Description

References

Mice

Lewis lung carcinoma model

Intraperitoneal injection

10 mg/kg

Twice daily

Enhanced anti-PD-1 therapy efficacy

J Hematol Oncol. 2020 Jul 20;13(1):99.

Mice

Xenograft model

Intraperitoneal injection

10 mg/kg

Twice daily for 4 weeks

To evaluate tumor growth inhibition and assess the tumor-suppressive function of THZ1.

Cancer Res. 2017 Dec 1;77(23):6614-6626.

Mice

U251-luc orthotopic xenograft model

IntratumOral injection

10 mg/kg

Continuous infusion for 4 weeks

To evaluate the effect of SNS032 on the growth of orthotopic U251-luc tumors, results showed that SNS032 significantly inhibited tumor growth and extended the survival of mice.

Neuro Oncol. 2024 Jan 5;26(1):70-84.

NOD/SCID-γ mice

Systemic U266 xenograft model

Intraperitoneal injection

10 mg/kg

Once daily, 5 days/week for 4 weeks

THZ1 significantly reduced tumor burden and prolonged survival with minimal toxicity

Clin Cancer Res. 2019 Oct 15;25(20):6195-6205.

(E/Z)-THZ1 2HCl 动物研究

Dose

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

Administration

i.p., i.v.

(E/Z)-THZ1 2HCl 参考文献

(E/Z)-THZ1 2HCl 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 2HCl 技术信息

CAS号	2095433-94-4
分子式	C₃₁H₃₀Cl₃N₇O₂
分子量	638.97
SMILES Code	O=C(NC1=CC=CC(NC2=NC=C(Cl)C(C3=CNC4=C3C=CC=C4)=N2)=C1)C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5.[H]Cl.[H]Cl
MDL No.	N/A

别名	THZ1 Dihydrochloride; THZ1 2HCl
运输	蓝冰
InChI Key	AJTGQOACYBCREM-QVLKBJGCSA-N
Pubchem ID	129896819

存储条件	In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C

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