KSQ 4279 最新

Cat. No. 7746 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective USP1 allosteric inhibitor

别名： Ubiquitin-specific Protease 1 Inhibitor 1,USP1-IN-1,USP1 Inhibitor 1,RO7623066

化学名： 6-(4-Cyclopropyl-6-methoxypyrimidin-5-yl)-1-(4-(1-isopropyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-1H-pyrazolo[3,4-d]pyrimidine

纯度： ≥98% (HPLC)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for KSQ 4279

KSQ 4279 is a potent and selective allosteric inhibitor of the ubiquitin specific protease 1 (USP1) (IC₅₀ = 11 nM; Ki = 1.2 nM), a key regulator of DNA damage repair pathway (distinct from PARP inhibitors). It displays selectivity for USP1 over other USP, UCH and OTU enzymes.

KSQ 4279 has strong antiproliferation effects in vitro. It induces accumulation of mono-ubiquitinated substrates in MDA-MB-436 cells.

In vivo, KSQ 4279 induces anti-tumor response in the BRCA1 mutant ovarian PDX model (mouse). It also displays synergistic effects with PARP inhibitor Olaparib (Cat. No. 7579) leading to significant and durable anti-tumor response in mice. KSQ 4279 is orally bioavailable.

技术数据 for KSQ 4279

分子量	534.54
公式	C₂₇H₂₅F₃N₈O
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	2446480-97-1
PubChem ID	150782011
InChI Key	KCBWAFJCKVKYHO-UHFFFAOYSA-N
Smiles	FC(F)(C1=CN(C(C)C)C(C2=CC=C(CN3N=CC4=C3N=C(C5=C(C6CC6)N=CN=C5OC)N=C4)C=C2)=N1)F

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for KSQ 4279

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	53.45	100
	ethanol	53.45	100

制备储备液 for KSQ 4279

以下数据基于产品分子量 534.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.87 mL	9.35 mL	18.71 mL
5 mM	0.37 mL	1.87 mL	3.74 mL
10 mM	0.19 mL	0.94 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

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产品说明书 for KSQ 4279

分析证书/产品说明书

化学品安全技术说明书

参考文献 for KSQ 4279

参考文献是支持产品生物活性的出版物。

Nusawardhana et al (2024) USP1-dependent nucleolytic expansion of PRIMPOL-generated nascent DNA strand discontinuities during replication stress. Nucleic Acids Research 52 2340 PMID: 38180818

Li et al (2024) Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors. Eur.J.Med.Chem. 275 116568 PMID: 38889606

Cadzow et al (2024) The USP1 inhibitor KSQ-4279 overcomes PARP inhibitor resistance in homologous recombination-deficient tumors. Cancer Res. 84 3419 PMID: 39402989

If you know of a relevant reference for KSQ 4279, please let us know.

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关键词: KSQ 4279, KSQ 4279 supplier, KSQ, 4279, potent, selective, inhibitor, inhibits, USP1, ubiquitin, specific, allosteric, damage, repair, pathway, DUB, PARP1, antiproliferation, antitumor, cancer, synergistic, olaparib, in, vivo, orally, bioavailable, Ubiquitin-specific, Protease, 1, Inhibitor, USP1-IN-1, RO7623066, Deubiquitinating, Enzymes, 7746, Tocris Bioscience

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