CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
| Molecular Weight | 291.8 |
| Formula | C14H14ClN3S |
| CAS Number | 357649-93-5 |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Claudia Canzonetta, et al. SAGA complex and Gcn5 are necessary for respiration in budding yeast
| Related Histone Acetyltransferase Products |
|---|
| AU-18069
AU-18069 is a CBP/p300 HAT inhibitor that can be used in studies related to hematological and solid tumors. |
| KAT modulator-1
KAT modulator-1 is a KAT modulator. |
| KAT6-IN-1
KAT6-IN-1 is a potent KAT6 inhibitor. |
| MC4171
MC4171 is a selective KAT8 inhibitor (IC50=8.1 µM). |
| MOZ-IN-3
MOZ-IN-3 is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
