PRMT5-IN-30

Cat. No.: HY-Q36691 Purity: 99.17%: Data Sheet
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PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 0.33 μM and a K_d of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation.

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

PRMT5-IN-30 Chemical Structure

CAS No. : 330951-01-4

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	Get quote
10 mg	Get quote

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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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PRMT5

0.33 μM (IC₅₀)

PRMT5

0.987 μM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 100 μM Compound: 17	Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA	[PMID: 28650658]
HEK293	IC₅₀	0.33 μM Compound: 17	Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth	[PMID: 28650658]
JeKo-1	EC₅₀	15 μM Compound: 17	Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay	[PMID: 28650658]
KOPN-8	EC₅₀	15 μM Compound: 17	Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay	[PMID: 28650658]
MV4-11	EC₅₀	25.73 μM Compound: 17	Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay	[PMID: 28650658]
MV4-11	EC₅₀	6.53 μM Compound: 17	Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay	[PMID: 28650658]
MV4-11	EC₅₀	80.74 μM Compound: 17	Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay	[PMID: 28650658]
Z-138	EC₅₀	15 μM Compound: 17	Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay	[PMID: 28650658]

Molecular Weight

371.41

Formula

C₁₈H₁₇N₃O₄S

CAS No.

330951-01-4

Appearance

Solid

Color

White to off-white

SMILES

C1(SCC(=O)NC2C=CC=CC=2C(OC)=O)NC2C(=CC=C(OC)C=2)N=1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (134.62 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	2.6924 mL	13.4622 mL	26.9244 mL
5 mM	0.5385 mL	2.6924 mL	5.3849 mL
10 mM	0.2692 mL	1.3462 mL	2.6924 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
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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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In Vivo Dissolution Calculator

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.17%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (249 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Ruifeng Mao, et al. Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. J Med Chem. 2017 Jul 27;60(14):6289-6304. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6924 mL	13.4622 mL	26.9244 mL	67.3111 mL
	5 mM	0.5385 mL	2.6924 mL	5.3849 mL	13.4622 mL
	10 mM	0.2692 mL	1.3462 mL	2.6924 mL	6.7311 mL
	15 mM	0.1795 mL	0.8975 mL	1.7950 mL	4.4874 mL
	20 mM	0.1346 mL	0.6731 mL	1.3462 mL	3.3656 mL
	25 mM	0.1077 mL	0.5385 mL	1.0770 mL	2.6924 mL
	30 mM	0.0897 mL	0.4487 mL	0.8975 mL	2.2437 mL
	40 mM	0.0673 mL	0.3366 mL	0.6731 mL	1.6828 mL
	50 mM	0.0538 mL	0.2692 mL	0.5385 mL	1.3462 mL
	60 mM	0.0449 mL	0.2244 mL	0.4487 mL	1.1219 mL
	80 mM	0.0337 mL	0.1683 mL	0.3366 mL	0.8414 mL
	100 mM	0.0269 mL	0.1346 mL	0.2692 mL	0.6731 mL

PRMT5-IN-30 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-30330951-01-4Histone MethyltransferasePRMT5 inhibitorSmD3 methylationantitumor activityInhibitorinhibitorinhibit

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PRMT5-IN-30

PRMT5-IN-30 Related Antibodies

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Biological Activity

Purity & Documentation

References

Customer Review

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