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

PRMT5-IN-1 hydrochloride Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of PRMT5-IN-1 hydrochloride:

PRMT5-IN-1 hydrochloride 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 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

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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

PRMT5

 

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

469.32

Formula

C20H22Cl2N4O5
Appearance

Solid

Color

Off-white to pink

SMILES

O[C@@H]1[C@@H](O)[C@H](N2C=CC3=C2N=CN4C3=NCC4O)O[C@H]1C[C@H](C5=CC=C(Cl)C=C5)O.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 (266.34 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 2.1307 mL 10.6537 mL 21.3074 mL
5 mM 0.4261 mL 2.1307 mL 4.2615 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
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
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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mg/kg

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g

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(per animal)

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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 2.1307 mL 10.6537 mL 21.3074 mL 53.2686 mL
5 mM 0.4261 mL 2.1307 mL 4.2615 mL 10.6537 mL
10 mM 0.2131 mL 1.0654 mL 2.1307 mL 5.3269 mL
15 mM 0.1420 mL 0.7102 mL 1.4205 mL 3.5512 mL
20 mM 0.1065 mL 0.5327 mL 1.0654 mL 2.6634 mL
25 mM 0.0852 mL 0.4261 mL 0.8523 mL 2.1307 mL
30 mM 0.0710 mL 0.3551 mL 0.7102 mL 1.7756 mL
40 mM 0.0533 mL 0.2663 mL 0.5327 mL 1.3317 mL
50 mM 0.0426 mL 0.2131 mL 0.4261 mL 1.0654 mL
60 mM 0.0355 mL 0.1776 mL 0.3551 mL 0.8878 mL
80 mM 0.0266 mL 0.1332 mL 0.2663 mL 0.6659 mL
100 mM 0.0213 mL 0.1065 mL 0.2131 mL 0.5327 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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