PRMT5-IN-1 hydrochloride

Name: PRMT5-IN-1 hydrochloride
Brand: MedChemExpress
SKU: HY-126256A
Rating: 4.5 (1 reviews)

Cat. No.: HY-126256A Purity: 99.50%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

PRMT5-IN-1 hydrochloride Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 582	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 2050	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 4150	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PRMT5-IN-1 hydrochloride:

PRMT5-IN-1 Get quote

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

In Vitro

PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits the PRMT5/MEP50 complex [K_inact/K_I=1.2×10⁵ M^-1 min^-1] very rapidly with a K_inact of 0.068 min^-1 and a good binding affinity (K_I=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.

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
10 mM	0.2196 mL	1.0982 mL	2.1964 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

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Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.50%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (253 KB) HNMR (276 KB) LCMS (243 KB)

Handling Instructions (2659 KB)

References

[1]. Lin H, et, al. Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors. ACS Med Chem Lett. 2019 May 22;10(7):1033-1038. [Content Brief]

Complete Stock Solution Preparation Table

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