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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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 |
| 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 |
|
| 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 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
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