2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT5-IN-1

PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PRMT5-IN-1 hydrochloride) usually boasts enhanced water solubility and stability.

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PRMT5-IN-1 Chemical Structure

PRMT5-IN-1 Chemical Structure

CAS No. : 2366149-83-7

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Other Forms of PRMT5-IN-1:

PRMT5-IN-1 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D 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-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].

IC50 & Target[1]

PRMT5

 

Cellular Effect
Cell Line Type Value Description References
Granta-519 IC50
0.012 μM
Compound: 9
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
[PMID: 31312404]
Granta-519 IC50
0.06 μM
Compound: 9
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
[PMID: 31312404]
In Vitro

PRMT5 IN-1 (0-500 nM) inhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105 M-1 min-1] very rapidly with a Kinact of 0.068 min-1 and a good binding affinity (KI=55 nM)[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM[1].

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

PRMT5-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: Granta-519 cells
Concentration: 0, 0.0001524, 0.000457, 0.001372, 0.004115, 0.012346, 0.037037, 0.111111, 0.333333 and 1 μM
Incubation Time: 10 days
Result: Inhibited cell proliferative, in which cells died on day 10 at high concentrations (0.3 and 1 μM).

Western Blot Analysis[1]

Cell Line: Granta-519 cells
Concentration: 0, 0.05, 0.15, 0.46, 1.37, 4, 12, 37, 111, 333, 1000 nM
Incubation Time: 3 days
Result: Inhibited cellular sDMA in Granta-519 cells in a dose-dependent manner.
Molecular Weight

418.83

Formula

C19H19ClN4O5
CAS No.
SMILES

O[C@@H]1[C@@H]([C@@H](C2=CC=C(Cl)C=C2)O)O[C@@H](N3C=CC4=C3N=CN5C4=NCC5O)[C@@H]1O
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-1 Related Classifications

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The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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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-12366149-83-7Histone MethyltransferasehemiaminalaldehydesC449cellular sDMAGranta-519 cellsanticancerInhibitorinhibitorinhibit

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