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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-SKLB06489
SKLB06489

Chemical Structure : SKLB06489

CAS No.:

SKLB06489 (SKLB-06489)

货号: PC-25966Not For Human Use, Lab Use Only.

SKLB06489 is a potent, selective type I PRMTs inhibitor with IC50 of 64.55, 4.21, and 51.27 nM for PRMT1, PRMT6, and PRMT8 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SKLB06489 is a potent, selective type I PRMTs inhibitor with IC50 of 64.55, 4.21, and 51.27 nM for PRMT1, PRMT6, and PRMT8 respectively.
SKLB06489 dose-dependently inhibits cell proliferation and colony formation with IC50 values in the low micromolar range in TNBC cell lines MDA-MB-231, Hs578T, and BT549.
SKLB06489 (40, 80 mg·kg-1·d-1, i.g. for 33 days) dose-dependently suppressed tumor growth in MDA-MB-231 subcutaneous xenograft models.
SKLB06489 inhibited TNBC proliferation by impairing DNA replication, compromising DNA damage repair, and ultimately inducing G0/G1-phase cell cycle arrest and apoptosis.
SKLB06489 (5, 10 μΜ) dose-dependently enhanced intracellular cholesterol efflux in MDA-MB-231 cells and Hs578T cells via upregulation of the ATP-binding cassette transporter A1 (ABCA1) and ATP-binding cassette transporter G1 (ABCG1), thereby disrupting cholesterol metabolic homeostasis.

物理化学性质&存储条件

分子量 419.57
分子式 C25H33N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(3-((methyl(2-(methylamino)ethyl)amino)methyl)-1H-indazol-5-yl)phenyl)cyclohexanecarboxamide

参考文献

1. Zhou SY, et al. Acta Pharmacol Sin. 2026 Jan 16. doi: 10.1038/s41401-025-01713-5.

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