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PRMT5-IN-53 is an orally active, gut-restricted PRMT5 inhibitor, exhibiting pIC50 values of ≥ 9.7 against both hPRMT5 and mPRMT5. It binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. In mice, PRMT5-IN-53 effectively inhibits intestinal PRMT5, significantly reducing both the number and size of polyps while avoiding systemic hematologic toxicity such as anemia and neutropenia. This compound is applicable in colorectal cancer research, particularly for familial adenomatous polyposis (FAP).
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PRMT5-IN-53 is an orally active, gut-restricted PRMT5 inhibitor, exhibiting pIC50 values of ≥ 9.7 against both hPRMT5 and mPRMT5. It binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. In mice, PRMT5-IN-53 effectively inhibits intestinal PRMT5, significantly reducing both the number and size of polyps while avoiding systemic hematologic toxicity such as anemia and neutropenia. This compound is applicable in colorectal cancer research, particularly for familial adenomatous polyposis (FAP). |
| Targets&IC50 | PRMT5:≥ 9.7 (pIC50) |
| In vitro | PRMT5-IN-53 (Compound 9) inhibits global SDMA methylation in A549 cells with a pIC₅₀ value of 9.4 μM. |
| In vivo | PRMT5-IN-53 (Compound 9), administered at 25-75 mg/kg twice daily for 7 to 21 consecutive days, demonstrates significant pharmacological effects in the colon and shows efficacy in a DSS-induced Apc Min/+ mouse polyp model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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