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首页-小分子抑制剂&激动剂-Others-Other Targets-HKB99
HKB99

Chemical Structure : HKB99

CAS No.: 2414908-90-8

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HKB99 (PGAM1 allosteric inhibitor HKB99)

货号: PC-72381Not For Human Use, Lab Use Only.

HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.
HKB99 significantly inhibited the proliferation of NSCLC cells (PC9, HCC827, H1975, and A549) in a concentration-dependent manner with the IC50 of 17-67 uM.
HKB99 allosterically block conformational change of PGAM1 during catalytic process and PGAM1-ACTA2 interaction, disrupts cellular migration and induces apoptosis in NSCLC cells.
HKB99 resensitizes the erlotinib-resistant NSCLC cells to erlotinib treatment. HKB99 (100 mg/kg, i.p.) significantly suppresses tumor growth and augments the tumoricidal effect of erlotinib in mouse xenografts

物理化学性质&存储条件

分子量 450.465
分子式 C23H18N2O6S
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

4-(azetidin-1-yl)-N-(3,4-dihydroxy-9,10-dioxo-9,10-dihydroanthracen-2-yl)benzenesulfonamide

参考文献

1. Huang K, et al. Cell Metab. 2019 Dec 3;30(6):1107-1119.e8.

2. Liang Q, et al. Acta Pharmacol Sin. 2021 Jan;42(1):115-119.

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