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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA/RNA Synthesis-Novobiocin
Novobiocin

Chemical Structure : Novobiocin

CAS No.: 303-81-1

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Novobiocin (Albamycin, Cathomycin)

货号: PC-49690Not For Human Use, Lab Use Only.

Novobiocin (NVB) is a potent, specific DNA polymerase theta (POLθ, POLQ) inhibitor with IC50 of 24 uM, selectively kills HR-deficient tumor cells in vitro and in vivo.

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50 mg ￥1980 In stock
100 mg ￥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Novobiocin (NVB) is a potent, specific DNA polymerase theta (POLθ, POLQ) inhibitor with IC50 of 24 uM, selectively kills HR-deficient tumor cells in vitro and in vivo.
Novobiocin displays no activity agaginst six other DNA repair related enzymes HSP90AA1, TRIP13, BLM, RAD51, SMARCAL1 and CHD1.
Novobiocin binds directly and specifically to the POLθ ATPase domain in vitro.
Novobiocin impairs POLθ DNA repair function and phenocopies POLθ depletion in human celsl.
Novobiocin strongly and specifically suppresses the growth of HR-deficient tumors in vivo, Novobiocin (75 mg/kg, via IP, b.i.d.) kills HR-deficient tumors and overrides PARPi resistance in vivo in PDX models.
Novobiocin induces excessive DSB end resection and non-productive RAD51 foci in U2OS cells, overcomes multiple PARPi resistance mechanisms.

物理化学性质&存储条件

分子量 612.63
分子式 C31H36N2O11
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

Benzamide, N-[7-[[3-O-(aminocarbonyl)-6-deoxy-5-C-methyl-4-O-methyl-alpha-L-lyxo-hexopyranosyl]oxy]-4-hydroxy-8-methyl-2-oxo-2H-1-benzopyran-3-yl]-4-hydroxy-3-(3-methyl-2-butenyl)-

参考文献

1. Zhou J, et al. Nat Cancer. 2021 Jun;2(6):598-610.

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