H-1152 2HCl | H-1152 dihydrochloride | ROCK Inhibitor | AmBeed-信号通路专用抑制剂

H-1152 2HCl {[allProObj[0].p_purity_real_show]}

货号：A747327 同义名： H-1152 dihydrochloride

H-1152 2HCl是一种选择性 ROCK 抑制剂，Ki 值为 1.6 nM，对 ROCK2 的 IC50 为 12 nM，且对其他激酶抑制作用较弱，广泛应用于细胞信号传导研究。

H-1152 2HCl 化学结构
CAS号：871543-07-6

H-1152 2HCl 3D分子结构
CAS号：871543-07-6

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H-1152 2HCl 纯度/质量文件产品仅供科研

货号：A747327 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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

H-1152 2HCl 质控信息

ROCK 亚型比较

产品名称	ROCK ↓ ↑	ROCK1 ↓ ↑	ROCK2 ↓ ↑	其他靶点	纯度
Thiazovivin	+ ROCK, IC50: ~0.5 μM				98%
Netarsudil HCl	++++ ROCK, Ki: 2 nM				99%+
Y-33075 2HCl	++++ ROCK, IC50: 3.6 nM				99%+
ROCK1-IN-1	++ ROCK, Ki: 17nM				95%
GSK429286A		+++ ROCK1, IC50: 14 nM	++ ROCK2, IC50: 63 nM		99%+
Ripasudil		++ ROCK1, IC50: 51 nM	++ ROCK2, IC50: 19 nM		99%+
Belumosudil			++ ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM		99%+
Y-27632 2HCl		++ ROCK1, Ki: 140 nM	+ ROCK2, Ki: 300 nM		99%+
Fasudil HCl			+ ROCK2, Ki: 330 nM	Rho,PKG	98%
Chroman 1		++++ ROCK1, IC50: 52 pM	++++ ROCK2, IC50: 1 pM		99%
BAY-549		++++ ROCK1, IC50: 0.6 nM	++++ ROCK2, IC50: 1.1 nM		99%+
AT13148		+++ ROCK1, IC50: 6 nM	+++ ROCK2, IC50: 4 nM	PKA	95%
RKI-1447		+++ ROCK1, IC50: 14.5 nM	+++ ROCK2, IC50: 6.2 nM		99%+
Hydroxyfasudil HCl		+ ROCK1, IC50: 0.73 μM	+ ROCK2, IC50: 0.72 μM	PKA	98%
H-1152 2HCl			+++ ROCK2, IC50: 0.0120 μM	PKG	99%
GSK269962A HCl		++++ ROCK1, IC50: 1.6 nM	+++ ROCK2, IC50: 4 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。

H-1152 2HCl 生物活性

靶点

ROCK2

ROCK2, IC50:0.0120 μM

描述

H-1152 dihydrochloride, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

H-1152 2HCl 细胞实验

Cell Line MDA-MB-468 cells MCF10A cells PC-12 cells MDA-MB-231 cells H2373 cells human umbilical vein endothelial cells (HUVECs) human umbilical vein endothelial cells (HUVECs) coronary arterioles PC-12 cells human dermal microvascular endothelial cells (HMVECs) INSw/GFPHES3 cells HUES8 cells TKCC5 human PDAC cells KPC mouse PDAC cells hippocampal neurons	Concentration	Treated Time	Description	References
MDA-MB-468 cells	1 μM	24 hours	inhibited TEAD reporter activity and cell proliferation	Nat Commun. 2022 Feb 4;13(1):703
MCF10A cells	1 μM	24 hours	inhibited TEAD reporter activity	Nat Commun. 2022 Feb 4;13(1):703
PC-12 cells	10 µM	24 hours	Induced neurite outgrowth, formed fully extended neurites	Cell Mol Biol Lett. 2006;11(1):12-29
MDA-MB-231 cells	1 μM	24 hours	inhibited TEAD reporter activity and cell proliferation	Nat Commun. 2022 Feb 4;13(1):703
H2373 cells	1 μM	24 hours	inhibited TEAD reporter activity and cell proliferation	Nat Commun. 2022 Feb 4;13(1):703
human umbilical vein endothelial cells (HUVECs)	3 µM	30 minutes	Inhibited ROCK activity, reversed CCM2 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability	J Exp Med. 2010 Apr 12;207(4):881-96
human umbilical vein endothelial cells (HUVECs)	3 µM	30 minutes	Inhibited ROCK activity, reversed KRIT1 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability	J Exp Med. 2010 Apr 12;207(4):881-96
coronary arterioles	10^-8 M	60 minutes	H-1152 alleviated oxidative stress and abolished enhanced vasoconstriction to ET-1 by inhibiting the ROCK signaling pathway.	Cardiovasc Res. 2017 Sep 1;113(11):1329-1337
PC-12 cells	1 µM	5-30 minutes	Induced neurite outgrowth, observed rapid cell shape change and neurite formation	Cell Mol Biol Lett. 2006;11(1):12-29
human dermal microvascular endothelial cells (HMVECs)	20 μmol/L	0.5 hours	H-1152 attenuated the AGE-induced alteration in monolayer permeability and cytoskeleton	Cardiovasc Diabetol. 2012 Jan 17;11:7
INSw/GFPHES3 cells	10 μM	8 days	Promote the generation and maturation of beta-like cells in three-dimensional culture, H1152 treatment significantly increases the percentage of INS+ cells and the expression of mature beta cell markers	Nat Commun. 2017 Aug 21;8(1):298
HUES8 cells	10 μM or 1 μM	4 days	Promote the generation of insulin-expressing cells from pancreatic progenitors, H1152 treatment significantly increases the percentage of INS+ cells	Nat Commun. 2017 Aug 21;8(1):298
TKCC5 human PDAC cells	10 µM	1 hour	Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1	Cancer Res. 2018 Jun 15;78(12):3321-3336
KPC mouse PDAC cells	10 µM	1 hour	Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1	Cancer Res. 2018 Jun 15;78(12):3321-3336
hippocampal neurons	100 nM	60 minutes	blocking the RhoA effector ROCK to prevent CRH-induced loss of thin dendritic spines	Mol Psychiatry. 2013 Apr;18(4):485-96

Cell Line

Concentration

Treated Time

Description

References

MDA-MB-468 cells

1 μM

24 hours

inhibited TEAD reporter activity and cell proliferation

Nat Commun. 2022 Feb 4;13(1):703

MCF10A cells

1 μM

24 hours

inhibited TEAD reporter activity

Nat Commun. 2022 Feb 4;13(1):703

PC-12 cells

10 µM

24 hours

Induced neurite outgrowth, formed fully extended neurites

Cell Mol Biol Lett. 2006;11(1):12-29

MDA-MB-231 cells

1 μM

24 hours

inhibited TEAD reporter activity and cell proliferation

Nat Commun. 2022 Feb 4;13(1):703

H2373 cells

1 μM

24 hours

inhibited TEAD reporter activity and cell proliferation

Nat Commun. 2022 Feb 4;13(1):703

human umbilical vein endothelial cells (HUVECs)

3 µM

30 minutes

Inhibited ROCK activity, reversed CCM2 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability

J Exp Med. 2010 Apr 12;207(4):881-96

human umbilical vein endothelial cells (HUVECs)

3 µM

30 minutes

Inhibited ROCK activity, reversed KRIT1 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability

J Exp Med. 2010 Apr 12;207(4):881-96

coronary arterioles

10^-8 M

60 minutes

H-1152 alleviated oxidative stress and abolished enhanced vasoconstriction to ET-1 by inhibiting the ROCK signaling pathway.

Cardiovasc Res. 2017 Sep 1;113(11):1329-1337

PC-12 cells

1 µM

5-30 minutes

Induced neurite outgrowth, observed rapid cell shape change and neurite formation

Cell Mol Biol Lett. 2006;11(1):12-29

human dermal microvascular endothelial cells (HMVECs)

20 μmol/L

0.5 hours

H-1152 attenuated the AGE-induced alteration in monolayer permeability and cytoskeleton

Cardiovasc Diabetol. 2012 Jan 17;11:7

INSw/GFPHES3 cells

10 μM

8 days

Promote the generation and maturation of beta-like cells in three-dimensional culture, H1152 treatment significantly increases the percentage of INS+ cells and the expression of mature beta cell markers

Nat Commun. 2017 Aug 21;8(1):298

HUES8 cells

10 μM or 1 μM

4 days

Promote the generation of insulin-expressing cells from pancreatic progenitors, H1152 treatment significantly increases the percentage of INS+ cells

Nat Commun. 2017 Aug 21;8(1):298

TKCC5 human PDAC cells

10 µM

1 hour

Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1

Cancer Res. 2018 Jun 15;78(12):3321-3336

KPC mouse PDAC cells

10 µM

1 hour

Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1

Cancer Res. 2018 Jun 15;78(12):3321-3336

hippocampal neurons

100 nM

60 minutes

blocking the RhoA effector ROCK to prevent CRH-induced loss of thin dendritic spines

Mol Psychiatry. 2013 Apr;18(4):485-96

H-1152 2HCl 动物实验

Species SCID mice SCID-beige mice	Animal Model Breast tumor xenograft model Diabetes model	Administration	Dosage	Frequency	Description	References
SCID mice	Breast tumor xenograft model	Intraperitoneal injection	25 mg/kg	Once daily for 31 days	Inhibited tumor growth	Nat Commun. 2022 Feb 4;13(1):703
SCID-beige mice	Diabetes model	Subrenal capsule transplantation	10 μM	Single transplantation, observed up to 4.5 months post-transplantation	Evaluate the function of H1152-treated beta-like cells in vivo, results show that H1152-treated cells have improved capacities to respond to glucose stimulation and maintain glucose homeostasis	Nat Commun. 2017 Aug 21;8(1):298

Species

SCID mice SCID-beige mice

Animal Model

Breast tumor xenograft model Diabetes model

Administration

Dosage

Frequency

Description

References

SCID mice

Breast tumor xenograft model

Intraperitoneal injection

25 mg/kg

Once daily for 31 days

Inhibited tumor growth

Nat Commun. 2022 Feb 4;13(1):703

SCID-beige mice

Diabetes model

Subrenal capsule transplantation

10 μM

Single transplantation, observed up to 4.5 months post-transplantation

Evaluate the function of H1152-treated beta-like cells in vivo, results show that H1152-treated cells have improved capacities to respond to glucose stimulation and maintain glucose homeostasis

Nat Commun. 2017 Aug 21;8(1):298

H-1152 2HCl 参考文献

H-1152 2HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.49mL

5.10mL

2.55mL

H-1152 2HCl 技术信息

CAS号	871543-07-6
分子式	C₁₆H₂₃Cl₂N₃O₂S
分子量	392.34
SMILES Code	CC1=CN=CC2=C1C(S(=O)(N3[C@@H](C)CNCCC3)=O)=CC=C2.[H]Cl.[H]Cl
MDL No.	MFCD06411451

别名	H-1152 dihydrochloride
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 9 mg/mL(22.94 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 35 mg/mL(89.21 mM)，配合低频超声助溶

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

方案二

方案三

配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在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。

方案一

H-1152 2HCl {[allProObj[0].p_purity_real_show]}

H-1152 2HCl 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

H-1152 2HCl 质控信息

H-1152 2HCl 生物活性

H-1152 2HCl 细胞实验

H-1152 2HCl 动物实验

H-1152 2HCl 参考文献

H-1152 2HCl 实验方案

H-1152 2HCl 技术信息

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H-1152 2HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

H-1152 2HCl 质控信息

H-1152 2HCl 生物活性

H-1152 2HCl 细胞实验

H-1152 2HCl 动物实验

H-1152 2HCl 参考文献

H-1152 2HCl 实验方案

H-1152 2HCl 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

细胞研究

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