CPTH2 |
カタログ番号GC39365 |
CPTH2 は、強力なヒストン アセチルトランスフェラーゼ (HAT) 阻害剤です。 CPTH2 は、Gcn5 によるヒストン H3 のアセチル化を選択的に阻害します。 CPTH2 はアポトーシスを誘導し、アセチルトランスフェラーゼ p300 (KAT3B) の阻害により明細胞腎癌 (ccRCC) 細胞株の浸潤性を低下させます。
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Cas No.: 357649-93-5
Sample solution is provided at 25 µL, 10mM.
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor and selectively inhibits the acetylation of histone H3 by recombinant human Gcn5 in a substrate-competive manner. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].
[1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44. [2]. Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6.
Cas No. | 357649-93-5 | SDF | |
Canonical SMILES | ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1 | ||
Formula | C14H14ClN3S | M.Wt | 291.8 |
溶解度 | DMSO: 25 mg/mL (85.68 mM); Water: < 0.1 mg/mL (insoluble) | Storage | 4°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.427 mL | 17.135 mL | 34.27 mL |
5 mM | 0.6854 mL | 3.427 mL | 6.854 mL |
10 mM | 0.3427 mL | 1.7135 mL | 3.427 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
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