MS-453|MS453;MS 453

Cas No.:	2059892-29-2
Chemical Name:	N-(3-((6,7-dimethoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl)amino)propyl)acrylamide
Synonyms:	MS453;MS 453
SMILES:	C(NCCCNC1=C2C(=NC(N3CCCC3)=N1)C=C(OC)C(OC)=C2)(=O)C=C
Formula:	C₂₀H₂₇N₅O₃
M.Wt:	385.468
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, selective. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM; exhibits selectivity for SETD8 against 28 other methyltransferases; does not causes significant reduction in the H4K20me in HeLa cells at up to 10 uM; poor membrane permeability (4.4 nm/s) and high efflux ratio (137).

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47618	PRMT5-IN-10	PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
DC47617	EED ligand 1	EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
DC47615	PRMT5-IN-9	PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM.
DC47613	PRMT5-IN-12	PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5.
DC47612	PRMT5-IN-11	PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
DC47611	PRMT5-IN-14	PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
DC47610	PRMT5-IN-3	PRMT5-IN-3 is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
DC47609	PRMT1-IN-1	PRMT1-IN-1 is a PRMT1 inhibitor.
DC47608	EZH2-IN-2	EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
DC47264	MS67	MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.