3-Deazaneplanocin A hydrochloride（DZNep HCl） is a histone methyltransferase inhibitor; decreases global histone methylation. Inhibits EZH2 histone methyltransferase and s-adenosylhomocysteine (SAH) hydrolase activity. Blocks trimethylation of lysine 27 on histone H3 and lysine 20 on histone H4 in vitro. Induces apoptosis in multiple cancer cell lines and has no apoptotic effect on normal cells. Enhances Oct4 expression in chemically induced pluripotent stem cells (CiPSCs).
| Molecular Weight | 298.73 |
| Formula | C12H14N4O3.HCl |
| CAS Number | 120964-45-6 |
| Solubility (25°C) | Water 30 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.
| Related Histone Methyltransferase Products |
|---|
| SAH-EZH2
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. |
| UNC4976
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. |
| C21
C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC50 of 1.8 μM. |
| EZH2-IN-15
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. |
| NSD-IN-2
NSD-IN-2 is a potent and irreversible NSD1 inhibitor. |
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