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1430213-30-1

中文名稱 N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲
英文名稱 ML216
CAS 1430213-30-1
分子式 C15H9F4N5OS
分子量 383.32
MOL 文件 1430213-30-1.mol
更新日期 2024/12/18 10:22:36
1430213-30-1 結(jié)構(gòu)式 1430213-30-1 結(jié)構(gòu)式

基本信息

中文別名
BLM解螺旋酶抑制劑(ML216)
N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲
英文別名
ML216
CS-1561
CID49852229
CID-49852229
CID 49852229
ML216(CID4985229)
ML216(CID-49852229)
ML 216
ML-216
CID-49852229
CID49852229
CID 49852229
1-[4-Fluoro-3-(trifluoromethyl)phenyl]-3-[5-(4-pyridinyl)-1,3,4-t hiadiazol-2-yl]ure
N-[4-Fluoro-3-(trifluoromethyl)phenyl]-N'-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]urea
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

密度1.583±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO:29.0(Max Conc. mg/mL);75.65(Max Conc. mM)
酸度系數(shù)(pKa)6.40±0.50(Predicted)
形態(tài)粉末
顏色淺橙色至深橙色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301-H413
防范說(shuō)明P273-P301+P310+P330
危險(xiǎn)品標(biāo)志T
危險(xiǎn)類別碼25
安全說(shuō)明45
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1 / PGIII
WGK Germany3

常見(jiàn)問(wèn)題列表

生物活性
ML216 (CID-49852229)是一種有效地、選擇性地、具有抗腫瘤活性的 DNA unwinding activity of BLM(Bloom’s syndrome protein) 的抑制劑。ML216 抑制解旋酶BLM636-1298和BLMfull-length的IC50值分別為0.97 μM和2.98 μM。
靶點(diǎn)
TargetValue
BLM 636-1298
(Cell-free assay)
0.97 μM
BLM full-length
(Cell-free assay)
2.98 μM
體外研究

ML216 (12.5-50 μM; 24-72 hours; PSNG5 and PSNG13cells) treatment inhibits the proliferation of PSNF5 cells in a concentration-dependent manner, but not of PSNG13 cells.
ML216 treatment leads to a statistically significant increase in the frequency of sister chromatid exchanges (SCEs) in PSNF5 cells, but not in PSNG13 cells.
ML216 increases the sensitivity of PSNF5 cells to aphidicolin but has no sensitizing effect on isogenic PSNG13 cells devoid of BLM.
ML216 inhibits both the full length WRN ( IC 50 of 5 μM) and a truncated WRN 500-946 ( IC 50 of 12.6 μM), with the former being 2.5-fold more sensitive to inhibition. BLM is a little more sensitive than WRN to inhibition by ML216 (1.7-fold based on IC 50 values). Despite the detectable inhibition of WRN by ML216, this compound appears selective for BLM in human cells. ML216 inhibits proliferation of WRN + and WRN ? cells equally well, and similarly sensitized both cell types to aphidicolin.

Cell Proliferation Assay

Cell Line: PSNG5 and PSNG13cells
Concentration: 12.5 μM or 50 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Inhibited the proliferation of PSNF5 cells, but not of PSNG13 cells, and did so in a concentration-dependent manner.
體內(nèi)研究

Although ML216 inhibits unwinding by the sequence-related BLM and WRN helicases similarly in vitro, the apparent dependence on BLM for ML216 to exert its biological effects in human cells suggests BLM specificity for the drug’s mechanism of action in vivo. A co-crystal structure of BLM in complex with inhibitor would be informative. Cellular cues in vivo may induce a specific conformation of WRN that makes it resistant to ML216.

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