CCG-100602
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 9.8 μM for PC-3 prostate cancer cells
CCG-100602 is a Rho pathway inhibitor.
Rho, a member of the Ras superfamily of small GTP-binding proteins, plays a key role in various biological processes including microtubule dynamics, gene transcription, actin cytoskeleton organization, cell cycle progression, oncogenic transformation, as well as epithelial wound repair.
In vitro: CCG-100602 was developed as a CCG-1423 analog for improved selectivity, potency, and attenuated cytotoxicity. It was found that CCG-100602 was able to inhibit RhoA/C-mediated and SRF-driven luciferase expression in PC-3 prostate cancer cells. At 100 μM, CCG-100602 showed 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, having an superior efficacy-toxicity profile to that of CCG-1423 [1].
In vivo: To evaluate whether inhibition of SRF could protect podocytes from hyperglycaemia injury, daily ip administration of CCG-1423 was performed in DM rata. Results showed that CCG-1423 could ameliorate proteinuria dose-dependently. CCG-1423 at 0.02 mg/kg could significantly reduce the body weight, compared with the vehicle controls. In addition, the inhibition of SRF with CCG-1423 also significantly abrogated the reduction of synaptopodin expression and the induction of SRF,α-SMA, FSP-1 expression in renal cortex tissues [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Evelyn, C. R.,Bell, J.L.,Ryu, J.G., et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorganic & Medicinal Chemistry Letters 20, 665-672 (2010).
[2] Zhao L, Wang X, Sun L, Nie H, Liu X, Chen Z, Guan G. Critical role of serum response factor in podocyte epithelial-mesenchymal transition of diabetic nephropathy. Diab Vasc Dis Res. 2016 Jan;13(1):81-92.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 478.8 |
Cas No. | 1207113-88-9 |
Formula | C21H17ClF6N2O2 |
Solubility | ≥152.4 mg/mL in DMSO; ≥26.9 mg/mL in EtOH; insoluble in H2O |
Chemical Name | 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-3-piperidinecarboxamide |
SDF | Download SDF |
Canonical SMILES | ClC(C=C1)=CC=C1NC(C(C2)CCCN2C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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