2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT5-IN-53

PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP).

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PRMT5-IN-53

PRMT5-IN-53 Chemical Structure

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PRMT5-IN-53 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP)[1].

IC50 & Target[1]

PRMT5

≥ 9.7 (pIC50)

In Vitro

PRMT5-IN-53 (Compound 9) inhibits global SDMA methylation in A549 cells with an pIC50 value of 9.4 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PRMT5-IN-53 Related Antibodies
In Vivo

PRMT5-IN-53 (Compound 9) (25-75 mg/kg, i.g., twice daily for 7-21 days) exhibits significant colonic pharmacological effects and displays efficacy in an established polyp DSS (HY-116282C)-treated ApcMin/+ mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DSS-induced polyp-bearing model established in Female ApcMin/+ (C57BL/6J-ApcMin/J, aged 4−5 weeks)[1]
Dosage: 25 and 75 mg/kg
Administration: Intragastric administration (i.g.), twice daily for 14-21 days
Result: Significantly reduced SDMA and SmD3-Me2 during 2 weeks in the colon tissue, bone marrow and spleen showed no changes in SDMA signals during 1 week.
Reduce the number and size of polyps during 3 weeks.
Did not cause systemic targeted toxicity.
Molecular Weight

390.44

Formula

C21H22N6O2
SMILES

O[C@@H]1[C@H](O)[C@@H](CNC(C=C2)=CC3=C2C=CC(N)=N3)C[C@H]1N4C(N=CN=C5[H])=C5C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PRMT5-IN-53 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRMT5-IN-53Histone MethyltransferaseColorectal Cancer (CRC)Adenomatous Polyposis Coli (APC)Familial Adenomatous PolyposisSymmetrical DimethylargininePharmacokinetics (PK)Inhibitorinhibitorinhibit

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