| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
CCG-100602 targets the myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling pathway. More specifically, it inhibits the nuclear translocation of MRTF-A, a coactivator of SRF. SRF is a transcription factor that regulates the expression of numerous genes involved in cell proliferation, migration, and differentiation, including many that are critical for fibrogenesis. By blocking MRTF-A from entering the nucleus, CCG-100602 prevents the formation of the MRTF-A/SRF transcriptional complex, thereby inhibiting the expression of SRF target genes. This pathway is downstream of Rho GTPase signaling, making CCG-100602 an effective tool for studying Rho-mediated cellular responses.
|
|---|---|
| ln Vitro |
CCG-100602 is a particular antagonist of the signaling pathway associated with myocardin-related transcription factor A/serum response factor (MRTF-A/SRF). By preventing MRTF-A from nuclear localization, it suppresses the fibrogenic transcription factor SRF.[2]
In vitro, CCG-100602 has demonstrated potent inhibitory activity on MRTF-A/SRF signaling. It specifically blocks the nuclear localization of MRTF-A, leading to the inhibition of SRF-mediated transcription. In cellular assays, CCG-100602 (3-30 μM) decreases the number of adherent human adipose-derived stem cells (hASC). It has also been shown to inhibit the expression of MRTF-A/SRF-activated genes. In HCT-116 human colon carcinoma cells, it exhibits an IC50 of 16.7 μM for antiproliferative activity. The compound effectively inhibits the fibrogenic transcription factor SRF, making it a valuable tool for studying fibrosis and related pathways. |
| ln Vivo |
CCG-100602 reduces arterial compliance and strain in spontaneously hypertensive rats, which reverses the increase in aortic stiffness. This suggests a strong anti-stiffening effect brought on by the inhibition of SRF/myocardin.[3]
In vivo activity data for CCG-100602 is limited in the available literature. As a specific inhibitor of the MRTF-A/SRF signaling pathway, it is primarily used as a research tool to study the consequences of inhibiting this pathway in various disease models. The compound's ability to block MRTF-A nuclear localization and inhibit SRF-mediated transcription suggests potential for in vivo applications in studying fibrosis and cancer. However, specific in vivo efficacy data is not extensively detailed. |
| Enzyme Assay |
The activity of CCG-100602 as an MRTF-A/SRF inhibitor is typically assessed using reporter gene assays that measure SRF-mediated transcription. These assays involve transfecting cells with a luciferase reporter construct driven by SRF response elements and treating them with the compound. The inhibition of SRF activity is then quantified by measuring luciferase activity. Additionally, the compound's ability to block MRTF-A nuclear localization can be confirmed using immunofluorescence microscopy, where cells are stained for MRTF-A and the nuclear/cytoplasmic distribution is assessed.
|
| Cell Assay |
After 7 days of culture in either basic culture medium (BM), osteogenic medium (OM), or adipogenic medium (AM) supplemented with 15, 20, 25, or 30 μM CCG-1423 or 3, 8, 15, or 30 μM CCG-100602 inhibitor, hASCs are subjected to A/D analysis. While a very small percentage of dead cells are stained with red dye, green dye indicates living cells.
In vitro cellular assays for CCG-100602 involve treating various cell lines with the compound and assessing its effects on cell viability, proliferation, and gene expression. The antiproliferative activity is commonly evaluated using CCK-8 or MTT assays, as demonstrated in HCT-116 cells where an IC50 of 16.7 μM was determined. The compound's effect on the expression of MRTF-A/SRF target genes, such as those involved in fibrosis and cytoskeletal regulation, is assessed by qRT-PCR or Western blot analysis. The inhibition of MRTF-A nuclear translocation can be visualized by immunofluorescence. |
| Animal Protocol |
Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats
7.5 mg/kg/day osmotic minipumps In vivo animal model protocols for CCG-100602 are not extensively detailed in the available literature. As a research compound targeting the MRTF-A/SRF pathway, it would typically be administered to animal models of fibrosis or cancer to evaluate its therapeutic potential. The compound's effects on disease progression, such as tumor growth or tissue fibrosis, would be assessed alongside pharmacodynamic markers of pathway inhibition. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for CCG-100602 is not extensively detailed in the available literature. As a small-molecule inhibitor, its pharmacokinetic properties would need to be evaluated in preclinical studies to determine parameters such as bioavailability, half-life, and tissue distribution. The compound is soluble in DMSO and is typically stored as a solid at -20°C for long-term stability.
|
| Toxicity/Toxicokinetics |
Specific toxicological data for CCG-100602 is not extensively detailed in the available literature. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development. The compound is a structural analog of CCG-1423, which was developed with improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound.
|
| References | |
| Additional Infomation |
Rho pathway inhibitors
CCG-100602 (CAS# 1207113-88-9) is a research compound used to study the Rho/MRTF/SRF signaling pathway. It is a specific inhibitor of MRTF-A/SRF-mediated transcription. The compound has a molecular formula of C21H17ClF6N2O2 and is supplied as a solid powder. It is not approved for clinical use and is intended for research purposes only. CCG-100602 is a valuable tool for investigating the role of the MRTF-A/SRF pathway in fibrosis, cancer, and other diseases. |
| Molecular Formula |
C21H17CLF6N2O2
|
|---|---|
| Molecular Weight |
478.82
|
| Exact Mass |
478.088
|
| Elemental Analysis |
C, 52.68; H, 3.58; Cl, 7.40; F, 23.81; N, 5.85; O, 6.68
|
| CAS # |
1207113-88-9
|
| Related CAS # |
1207113-88-9
|
| PubChem CID |
46190808
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
563.8±50.0 °C at 760 mmHg
|
| Flash Point |
294.8±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.544
|
| LogP |
5.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
32
|
| Complexity |
656
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(=CC=1)N(C(C1C=C(C(F)(F)F)C=C(C(F)(F)F)C=1)=O)C(C1CNCCC1)=O
|
| InChi Key |
MOQCFMZWVKQBAP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H17ClF6N2O2/c22-16-3-5-17(6-4-16)29-18(31)12-2-1-7-30(11-12)19(32)13-8-14(20(23,24)25)10-15(9-13)21(26,27)28/h3-6,8-10,12H,1-2,7,11H2,(H,29,31)
|
| Chemical Name |
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide
|
| Synonyms |
CCG100602; CCG 100602; CCG-100602
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~208.9 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0885 mL | 10.4423 mL | 20.8847 mL | |
| 5 mM | 0.4177 mL | 2.0885 mL | 4.1769 mL | |
| 10 mM | 0.2088 mL | 1.0442 mL | 2.0885 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
