BMH-21

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMH-21 是一种 RNA 聚合酶 I 抑制剂，在 NCI60 癌细胞系中具有广泛而有效的抗肿瘤活性，平均 GI50 为 160 nM。

BMH-21 is a RNA polymerase I inhibitor with wide and potent antitumorigenic activity across NCI60 cancer cell lines with mean GI50 of 160 nM, interacts with GC-Rich rDNA, potently and rapidly represses RNA polymerase I (Pol I) transcription; inhibits the expression of 47S rRNA transcript with IC50 of 60 nM, blocks transcription of the rRNA precursor without affecting rRNA maturation, and causes segregation of nucleolar proteins; causes proteasome-mediated degradation of RPA194 (Pol I catalytic subunit); activates p53 and inhibits TP53 null and mutant cell lines with GI50 of 110 and 205 nM, respectively.

BMH-21 binds ribosomal DNA and inhibits Pol I transcription.BMH-21 inhibits RNA polymerase I independent of DNA damage response.BMH-21 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences.BMH-21 (1 μM; 3 hours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation.Cell Viability AssayCell Line:U2OS cells Concentration:0 μM, 0.1 μM , 1 μM, 10 μM Incubation Time:48 hoursResult:Decreased the viability of cells at concentrations that activated the DNA damage response.Western Blot AnalysisCell Line:A375 cellsConcentration:1 μM Incubation Time:3 hours Result:Degraded RPA194 with blocked ATM and DNA-PKcs activity.

BMH-21 (50 mg/kg; i.p.; daily; for 6 days) inhibits HCT116 colon cancer tumor growth in vivo. Animal Model:6-week old athymic NCr nu/nu mice, with HCT116 colorectal carcinoma xenograft Dosage:50 mg/kg Administration:Intraperitoneal injection, daily, for 6 days Result:Significantly inhibited HCT116 colon cancer tumor growth.

BMH21

Cell Cycle/DNA Damage

DNA/RNA Synthesis

RNApolymeraseI

Cancer

——

896705-16-1

360.4091

C21H20N4O2

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC=CN2C1=NC3C=C(C=CC=C4)C4=CC3C2=O)NCCN(C)C

12H-Benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide, N-[2-(dimethylamino)ethyl]-12-oxo-

(-20℃)

With Ice Pack

≥ 2 years