CCG-100602
- CAS No.
- 1207113-88-9
- Chemical Name:
- CCG-100602
- Synonyms
- CCG-100602;CCG-100602 >=98% (HPLC);1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide;3-Piperidinecarboxamide, 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-;CCG 100602,Inhibitor,transcription,inhibit,serum,myocardin,nuclear,SRF,CCG100602,MRTF-A,CCG-100602,Ras,localization
- CBNumber:
- CB02590547
- Molecular Formula:
- C21H17ClF6N2O2
- Molecular Weight:
- 478.82
- MDL Number:
- MOL File:
- 1207113-88-9.mol
CCG-100602 price More Price(11)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2292 | CCG-100602 ≥98% (HPLC) | 1207113-88-9 | 5mg | $63.1 | 2024-03-01 | Buy |
Sigma-Aldrich | SML2292 | CCG-100602 ≥98% (HPLC) | 1207113-88-9 | 25mg | $179 | 2024-03-01 | Buy |
Cayman Chemical | 10787 | CCG-100602 ≥98% | 1207113-88-9 | 5mg | $38 | 2024-03-01 | Buy |
Cayman Chemical | 10787 | CCG-100602 ≥98% | 1207113-88-9 | 10mg | $71 | 2024-03-01 | Buy |
Cayman Chemical | 10787 | CCG-100602 ≥98% | 1207113-88-9 | 25mg | $166 | 2024-03-01 | Buy |
CCG-100602 Chemical Properties,Uses,Production
Uses
The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 μM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.[Cayman Chemical]
Biological Activity
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].
IC 50
9.8 μm for pc-3 prostate cancer cells
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.
CCG-100602 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4153 | 55 | |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9756 | 58 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
Energy Chemical | 021-58432009 400-005-6266 | marketing1@energy-chemical.com | China | 44894 | 58 |
MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8141 | 58 |