DS-437|cas 1674364-87-4|DC Chemicals

Cas No.:	1674364-87-4
Chemical Name:	1-[2-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylurea
Synonyms:	BDBM50089221;1-(2-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)ethyl)-3-ethylurea;5 inverted exclamation marka-S-[2-[[(Ethylamino)carbonyl]amino]ethyl]-5 inverted exclamation marka-thioadenosine;1-[2-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylure
SMILES:	S(C([H])([H])C([H])([H])N([H])C(N([H])C([H])([H])C([H])([H])[H])=O)C([H])([H])[C@]1([H])[C@]([H])([C@]([H])([C@]([H])(N2C([H])=NC3=C(N([H])[H])N=C([H])N=C23)O1)O[H])O[H]
Formula:	C₁₅H₂₃N₇O₄S
M.Wt:	397.4526
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	DS-437 is a potent, selective, dual inhibitor of PRMT5 and PRMT7 with IC50 of 6.0 uM for both, DS-437 is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases; inhibits methylation of full-length histone 4 by PRMT5-MEP50 with an IC50 of 37 ± 1.2 μM in a biochemical assay; inhibits symmetrical dimethylation of PRMT5 substrates in cells.
In Vivo:	DS-437 (10 mg/kg; i.p.; 5 times a week) has some beneficial effects on inhibiting tumor growth. The combination of DS-437 and the anti-p185erbB2/neu antibody 4D5 had even more dramatic effects[1]. Animal Model: Six to Ten weeks old female Balb/c mice (bearing CT26Her2 tumor cells)[1] Dosage: 10 mg/kg Administration: i.p.; 5 times a week Result: Had some beneficial effects on inhibiting tumor growth.
In Vitro:	DS-437 was able to inhibit methylation of an H4[1–24] peptide by the PRMT5–MEP50 complex under balanced conditions (cofactor and substrate concentrations set at their respective Km values) in a dose-dependent manner with an IC50 of 5.9 ± 1.4 μM[1]. DS-437 increased total CD8+ and CD8+ PD-1+ T cells[2].
References:	[1]. Smil D, et al. Discovery of a Dual PRMT5-PRMT7 Inhibitor.ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. [2]. Nagai Y, et al. PRMT5 Associates With the FOXP3 Homomer and When Disabled Enhances Targetedp185erbB2/neu Tumor Immunotherapy.Front Immunol. 2019 Feb 8;10:174.

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