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CCG-1423 {[allProObj[0].p_purity_real_show]}

货号:A381687

CCG-1423抑制 RhoA/C 介导的基因转录和 Rho 超表达细胞系的侵袭。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
CCG-1423 化学结构 CAS号:285986-88-1
CCG-1423 化学结构
CAS号:285986-88-1
CCG-1423 3D分子结构
CAS号:285986-88-1
CCG-1423 化学结构 CAS号:285986-88-1
CCG-1423 3D分子结构 CAS号:285986-88-1
规格 价格 会员价 库存 数量
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CCG-1423 纯度/质量文件 产品仅供科研

货号:A381687 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cdc42-subclass Rac Rho-subclass 其他靶点 纯度
ZCL278 ++

Cdc42 GTPase, Kd: 11.4 μM

98%
ML141 +++

cdc42, IC50: 200 nM

99%+
NSC 23766 3HCl +

Rac GTPase, IC50: 50 μM

98%
EHop-016 +++

Rac1, IC50: 1.1 μM

98%
Azathioprine 98%
EHT 1864 ++++

Rac1, Kd: 40 nM

Rac3, Kd: 50 nM

99%+
Zoledronic Acid Ras 98%
CCG-1423 99%+
CCG-203971 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。

CCG-1423 生物活性

靶点
  • Rho-subclass

描述 Rho GTPases are molecular switches that regulate many essential cellular processes, including actin dynamics, gene transcription, cell-cycle progression and cell adhesion[3]. Rho-kinase has pleiotropic functions including the regulation of cellular contraction, motility, morphology, polarity, cell division, and gene expression[4]. CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis. CCG-1423 selectively inhibited spontaneous PC-3 prostate cancer cell invasion through a Matrigel matrix in vitro, but not the Gαi-dependent LPA-stimulated SKOV-3 ovarian cancer cell invasion in vitro. At 100 μM, nearly complete inhibition of invasion was achieved with a lesser degree of toxicity than that induced by CCG-1423 at 10 μM[5]. Pharmacological SRF inhibition by CCG-1423 reduced nuclear MKL1 and improved glucose uptake and tolerance in insulin-resistant mice in vivo[6]. SRF binds to this site in vivo and the SRF inhibitor CCG-1423 completely blocks STARS proximal reporter activity in H9c2 cells[7]. Pharmacological MKL-inhibition with CCG-1423 significantly inhibited CCN1 promoter activity as well as mRNA and protein expression[8].

CCG-1423 细胞实验

Cell Line
Concentration Treated Time Description References
AGS 7.5 μM CCG-1423 effectively inhibited GC cells' invasion and MYH9 expression Theranostics. 2017 Aug 2;7(13):3338-3353.
MGC 80-3 7.5 μM CCG-1423 effectively inhibited GC cells' invasion and MYH9 expression Theranostics. 2017 Aug 2;7(13):3338-3353.
vascular smooth muscle cells 5 μM or 20 μM 24 h CCG-1423 inhibited H2O2-induced FOXM1 expression Redox Biol. 2023 Feb;59:102586.
vascular smooth muscle cells 5 μM or 20 μM 24 h CCG-1423 inhibited PDGF-induced FOXM1 expression Redox Biol. 2023 Feb;59:102586.
HEK293T cells 5 μM 4 h CCG-1423 significantly inhibited MICAL-2-induced SRF/MRTF-A reporter gene expression, reducing luciferase expression by 75%. Cell. 2014 Jan 30;156(3):563-76.
L6 myoblasts 1 μM CCG-1423 reversed palmitate-induced MKL1 nuclear localization, resulting in predominant localization of MKL1 to the cytosol. J Clin Invest. 2011 Mar;121(3):918-29.
L6 myotubes 1 μM 16 h CCG-1423 increased both basal and insulin-stimulated glucose uptake and blocked SRF activity by inhibiting MKL1 nuclear localization. J Clin Invest. 2011 Mar;121(3):918-29.
HmVEC 0.5, 1, 2.5, 5 µM 24 h CCG-1423 significantly inhibited the cord-forming ability of HmVEC, with 45% inhibition at 1 µM, 80% inhibition at 2.5 µM, and almost complete inhibition at 5 µM. Angiogenesis. 2017 Nov;20(4):663-672.
A10 VSMCs 0.1 μM 30 min CCG-1423 partially blocked the inhibitory effect of MYDGF on PDGF-BB-induced phenotypic switching in A10 VSMCs Acta Pharmacol Sin. 2024 Jan;45(1):98-111.
RH30 cells 10 µM 5 h CCG-1423 and PAX3-FOXO1 showed a significant synergistic effect in suppressing ACTA1 reporter activity. Cell Biosci. 2021 Jan 28;11(1):25.
TW03 80.55 μM 24 h CCG-1423 reversed the migration and invasion abilities of Nogo-B and NgR3, and downregulated the expression of N-Cadherin and MRTFA Cell Death Dis. 2022 Jan 24;13(1):76.
HK1 30.19 μM 24 h CCG-1423 reversed the migration and invasion abilities of Nogo-B and NgR3, and downregulated the expression of N-Cadherin and MRTFA Cell Death Dis. 2022 Jan 24;13(1):76.
RH30 cells 10 µM 5 h Observed significant synergistic effect between PAX3-FOXO1 and CCG-1423 to suppress ACTA1 reporter activity Cell Biosci. 2021 Jan 28;11(1):25.

CCG-1423 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice HFD-induced obese mice Intraperitoneal 0.15 mg/kg Once daily for 2 weeks CCG-1423 improved glucose tolerance in HFD-fed mice and decreased expression of SRF targets in skeletal muscle. J Clin Invest. 2011 Mar;121(3):918-29.
Nude mice Orthotopic-transplant nude-mouse models of GC Intraperitoneally 0.15 mg/kg Every 2 weeks for 2 weeks The tumor volumes of CCG-1423-treated group were smaller than the control group, and the metastatic nodules were also significantly less in CCG-1423-treated group Theranostics. 2017 Aug 2;7(13):3338-3353.
Mice Carotid artery ligation model Intraperitoneal injection 1 mg/kg Daily for 4 weeks CCG-1423 inhibited neointima formation after carotid artery ligation Redox Biol. 2023 Feb;59:102586.
Zebrafish Tg(kdrl:gfp)la116 zebrafish embryos Directly added to water 0.5, 1 µM 22 hours CCG-1423 at 1 μM significantly inhibited angiogenesis in zebrafish embryos, marked by reduced ISV (intersegmental vessel) formation and incomplete extension. Angiogenesis. 2017 Nov;20(4):663-672.
Mice CAP2-CKO mouse model Intraperitoneal injection 0.15 mg/kg Once daily for 21 days To evaluate the effect of CCG-1423-8u on cardiac function and survival in CAP2-CKO mice, results showed that CCG-1423-8u significantly extended survival and improved cardiac function JCI Insight. 2019 Mar 21;4(6):e124629

CCG-1423 参考文献

[1]Jin W, Goldfine AB, et al. Increased SRF transcriptional activity in human and mouse skeletal muscle is a signature of insulin resistance. J Clin Invest. 2011 Mar;121(3):918-29.

[2]Evelyn CR, Bell JL, et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorg Med Chem Lett. 2010 Jan 15;20(2):665-72.

[3]A L Bishop,et al. Rho GTPases and their effector proteins. Biochem J. 2000 Jun 1;348 Pt 2(Pt 2):241-55.

[4]Mutsuki Amano,et al. Rho-kinase/ROCK: A key regulator of the cytoskeleton and cell polarity. Cytoskeleton (Hoboken).2010 Sep;67(9):545-54.

[5]Evelyn CR, et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorg Med Chem Lett. 2010 Jan 15;20(2):665-72.

[6]Jin W, et al. Increased SRF transcriptional activity in human and mouse skeletal muscle is a signature of insulin resistance. J Clin Invest. 2011 Mar;121(3):918-29.

[7]Chong NW, et al. STARS is essential to maintain cardiac development and function in vivo via a SRF pathway. PLoS One. 2012;7(7):e40966.

[8]Duggirala A, et al. cAMP-induced actin cytoskeleton remodelling inhibits MKL1-dependent expression of the chemotactic and pro-proliferative factor, CCN1. J Mol Cell Cardiol. 2014 Nov 18;79C:157-168.

CCG-1423 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

21.99mL

4.40mL

2.20mL

CCG-1423 技术信息

CAS号285986-88-1
分子式C18H13ClF6N2O3
分子量 454.75
SMILES Code O=C(NOC(C)C(NC1=CC=C(Cl)C=C1)=O)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2
MDL No. MFCD01566719
别名
运输蓝冰
InChI Key DSMXVSGJIDFLKP-UHFFFAOYSA-N
Pubchem ID 2726015
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 105 mg/mL(230.9 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

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
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