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Thiazovivin {[allProObj[0].p_purity_real_show]}

货号:A211276

Thiazovivin是一种 ROCK 抑制剂,IC50 为 0.5 μM,在细胞外实验中促进人类胚胎干细胞的存活。

Thiazovivin 化学结构 CAS号:1226056-71-8
Thiazovivin 化学结构
CAS号:1226056-71-8
Thiazovivin 3D分子结构
CAS号:1226056-71-8
Thiazovivin 化学结构 CAS号:1226056-71-8
Thiazovivin 3D分子结构 CAS号:1226056-71-8
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Thiazovivin 纯度/质量文件 产品仅供科研

货号:A211276 标准纯度: {[allProObj[0].p_purity_real_show]}
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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, Ki: 41 nM

ROCK2, IC50: 60 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。

Thiazovivin 生物活性

靶点
  • ROCK

    ROCK, IC50:~0.5 μM

描述 Thiazovivin (GMP) is produced in accordance with GMP guidelines. GMP-compliant small molecules are effective as auxiliary reagents in the manufacture of cell therapies. Thiazovivin is recognized as a potent ROCK inhibitor[1].
体外研究

Thiazovivin, a ROCK inhibitor, at 2 μM, suppresses ROCK activity and enhances the survival of human embryonic stem cells (hESCs) post-dissociation without compromising their pluripotency. It strengthens cell-ECM adhesion via integrin signaling and stabilizes E-cadherin after cell dissociation, thereby protecting hESCs from death in ECM-free conditions[1].

Thiazovivin enhances the attachment and primary colony formation of embryo-derived stem-like cells (eSLCs) from cattle on feeder layers. It promotes colony outgrowth and facilitates the expansion of eSLC cultures during subculturing for passaging. Additionally, Thiazovivin increases the expression of ectodermal lineage-specific genes in cattle eSLCs[2].

Thiazovivin (GMP) (0.5 μM, at 1 day) effectively facilitates the rapid reprogramming of mouse tail tip and embryonic fibroblasts into iPSCs[1].

Thiazovivin (GMP) improves the efficiency of reprogramming endometrial adult stromal cells into iPSCs[2].

Thiazovivin (GMP) at 2 μM induces the formation of iPSCs and induced neural stem cells (iNSCs) from human urine cells (UCs)[3].

Thiazovivin (GMP) (2 μM, for the first 24 h) enhances the growth rate of hiPSCs[4].

Thiazovivin (GMP) at 0.5 μM, in combination with SB431542 and PD0325901, enhances iPSC reprogramming by regulating cell-cell interactions[5].

Thiazovivin 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
HSMCs 1 μM Function Assay 2 h reverses AngII-induced MYPT1 phosphorylation 24965170
SCU-i10 hiPSCs 0-20 μM Growth Inhibition Assay 24 h significantly modulates single-cell plating efficiency and promote NCM growth 25077932

Thiazovivin 动物研究

Dose Rat: 1 mg/kg - 30 mg/kg[3] (p.o.)
Administration p.o.

Thiazovivin 参考文献

[1]Xu Y, et al. Revealing a core signaling regulatory mechanism for pluripotent stem cell survival and self-renewal by small molecules. Proc Natl Acad Sci U S A. 2010 May 4;107(18):8129-34.

[2]Park S, et al. Thiazovivin, a Rho kinase inhibitor, improves stemness maintenance of embryo-derived stem-like cells under chemically defined culture conditions in cattle. Anim Reprod Sci. 2015 Oct;161:47-57.

[3]Cheng L, et al. Generation of Urine Cell-Derived Non-integrative Human iPSCs and iNSCs: A Step-by-Step Optimized Protocol. Front Mol Neurosci. 2017 Oct 30;10:348.

[4]Kuo HH, et al. Negligible-Cost and Weekend-Free Chemically Defined Human iPSC Culture. Stem Cell Reports. 2020 Feb 11;14(2):256-270.

[5]Lin T, et al. A chemical platform for improved induction of human iPSCs. Nat Methods. 2009 Nov;6(11):805-8.

Thiazovivin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL

Thiazovivin 技术信息

CAS号1226056-71-8
分子式C15H13N5OS
分子量 311.36
SMILES Code O=C(C1=CSC(NC2=NC=NC=C2)=N1)NCC3=CC=CC=C3
MDL No. MFCD16495823
别名
运输蓝冰
InChI Key DOBKQCZBPPCLEG-UHFFFAOYSA-N
Pubchem ID 46209426
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 30 mg/mL(96.35 mM),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

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
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

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