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
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- CAS號:
- 1430213-30-1
- 英文名:
- ML216
- 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
- 中文名:
- 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
- 中文別名:
- 化合物ML216;ML216,BLM 解旋酶抑制劑;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;1-(4-氟-3-(三氟甲基)苯基)-3-(5-(吡啶-4-基)-1,3,4-噻二唑-2-基)脲;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
- CBNumber:
- CB02715652
- 分子式:
- C15H9F4N5OS
- 分子量:
- 383.32
- MOL File:
- 1430213-30-1.mol
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N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲化學(xué)性質(zhì)
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密度:
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1.583±0.06 g/cm3(Predicted)
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儲存條件:
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2-8°C
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溶解度:
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DMSO:29.0(Max Conc. mg/mL);75.65(Max Conc. mM)
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酸度系數(shù)(pKa):
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6.40±0.50(Predicted)
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形態(tài):
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powder
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顏色:
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light orange to dark orange
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N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲性質(zhì)、用途與生產(chǎn)工藝
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。
| Target | Value |
BLM 636-1298
(Cell-free assay)
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0.97 μM
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BLM full-length
(Cell-free assay)
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2.98 μM
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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
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Cell Line:
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PSNG5 and PSNG13cells
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Concentration:
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12.5 μM or 50 μM
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Incubation Time:
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24 hours, 48 hours, 72 hours
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Result:
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Inhibited the proliferation of PSNF5 cells, but not of PSNG13 cells, and did so in a concentration-dependent manner.
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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.
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
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
|---|
| 2024/08/19 | HY-12342 | ML216 | | 1 mg | 250元 |
| 2024/08/19 | HY-12342 | 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
ML216 | 1430213-30-1 | 5mg | 550元 |
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
生產(chǎn)廠家
1430213-30-1, 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 相關(guān)搜索:
- 抑制劑
- 藥靶配體
- 細胞生物學(xué)試劑
- C15H9F4N5OS
- ML216,BLM 解旋酶抑制劑
- 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
- 化合物ML216
- 1-(4-氟-3-(三氟甲基)苯基)-3-(5-(吡啶-4-基)-1,3,4-噻二唑-2-基)脲
- 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
- 1430213-30-1
- helicase,CID 49852229,WRN,DNA,sister,inhibit,Anticancer,ML-216,anti-proliferative,DNA/RNA Synthesis,Inhibitor,chromatid,CID49852229,BLM,unwinding,toxicity,ML 216,ML216
- Urea, N-[4-fluoro-3-(trifluoromethyl)phenyl]-N'-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]-
- 1-[4-Fluoro-3-(trifluoromethyl)phenyl]-3-[5-(4-pyridinyl)-1,3,4-t hiadiazol-2-yl]ure
- ML216(CID4985229)
- ML216(CID-49852229)
- CS-1561
- ML 216; ML-216; CID-49852229; CID49852229; CID 49852229
- CID-49852229
- CID49852229
- CID 49852229
- N-[4-Fluoro-3-(trifluoromethyl)phenyl]-N'-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]urea
- 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
- ML216