PRMT5-IN-30

Cat. No.: HY-Q36691 Purity: 99.17%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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PRMT5-IN-30 Chemical Structure

CAS No. : 330951-01-4

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1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
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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 SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
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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

Purity & Documentation

Purity: 99.17%

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Data Sheet (268 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]

PRMT5-IN-30 Related Classifications

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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-30330951-01-4Histone MethyltransferasePRMT5 inhibitorSmD3 methylationantitumor activityInhibitorinhibitorinhibit

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