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

PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.

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PRMT5-IN-1 hydrochloride Chemical Structure

PRMT5-IN-1 hydrochloride Chemical Structure

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Based on 1 publication(s) in Google Scholar

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PRMT5-IN-1 hydrochloride Related Antibodies

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Description

PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].

IC50 & Target

IC50: 11 nM (PRMT5/MEP50)[1]
In Vitro

PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits 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) hydrochloride 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) hydrochloride 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 hydrochloride 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

455.29

Formula

C19H20Cl2N4O5
Appearance

Solid

Color

Off-white to pink

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.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (274.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1964 mL 10.9820 mL 21.9640 mL
5 mM 0.4393 mL 2.1964 mL 4.3928 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1964 mL 10.9820 mL 21.9640 mL 54.9101 mL
5 mM 0.4393 mL 2.1964 mL 4.3928 mL 10.9820 mL
10 mM 0.2196 mL 1.0982 mL 2.1964 mL 5.4910 mL
15 mM 0.1464 mL 0.7321 mL 1.4643 mL 3.6607 mL
20 mM 0.1098 mL 0.5491 mL 1.0982 mL 2.7455 mL
25 mM 0.0879 mL 0.4393 mL 0.8786 mL 2.1964 mL
30 mM 0.0732 mL 0.3661 mL 0.7321 mL 1.8303 mL
40 mM 0.0549 mL 0.2746 mL 0.5491 mL 1.3728 mL
50 mM 0.0439 mL 0.2196 mL 0.4393 mL 1.0982 mL
60 mM 0.0366 mL 0.1830 mL 0.3661 mL 0.9152 mL
80 mM 0.0275 mL 0.1373 mL 0.2746 mL 0.6864 mL
100 mM 0.0220 mL 0.1098 mL 0.2196 mL 0.5491 mL
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PRMT5-IN-1 hydrochloride Related Classifications

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-1Histone MethyltransferasehemiaminalaldehydesC449cellular sDMAGranta-519 cellsanticancerInhibitorinhibitorinhibit

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