ML216 is a potent inhibitor of the DNA unwinding activity of BLM helicase, showing similar IC50s of 3.0 and 0.97 μM for full length BLM and BLM636–1298 respectively.
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产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fexinidazole | ✔ | 98% | |||||||||||||||||
Daptomycin | ✔ | 98% | |||||||||||||||||
Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
Metronidazole | ✔ | 98% | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
Nedaplatin | ✔ | 99%+ | |||||||||||||||||
Oxolinic acid | ✔ | 98+% | |||||||||||||||||
Bendamustine | ✔ | 98+% | |||||||||||||||||
Trifluridine | ✔ | 98% | |||||||||||||||||
Robinetin | ✔ | 99%+ | |||||||||||||||||
Carboplatin | ✔ | 99% | |||||||||||||||||
Cidofovir | ✔ | 99% | |||||||||||||||||
Cisplatin | ✔ | 99% | |||||||||||||||||
Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
Oxaliplatin | ✔ | 98% | |||||||||||||||||
YK-4-279 | ✔ | 99%+ | |||||||||||||||||
ML216 |
+
BLMfull-length, IC50: 2.98 μM BLM636-1298, IC50: 0.97 μM |
99%+ | |||||||||||||||||
RK-33 | ✔ | 98% | |||||||||||||||||
Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
Phen-DC3 Trifluoromethanesulfonate | ✔ | 95% | |||||||||||||||||
Favipiravir | ✔ | 99% | |||||||||||||||||
Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
Didox | ✔ | 98% | |||||||||||||||||
(E)-3-AP | ✔ | 99% | |||||||||||||||||
Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
BC-LI-0186 |
+++
Leucyl-tRNA synthetase, IC50: 46.11 nM Leucyl-tRNA synthetase, Kd: 42.1 nM |
98% | |||||||||||||||||
SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | ML216 (CID-49852229) acts as a powerful, selective, and cell-penetrable blocker of BLM helicase's DNA unwinding function, exhibiting IC50 values of 2.98 μM for BLM full-length and 0.97 μM for BLM636-1298. Additionally, ML216 suppresses BLM's ssDNA-dependent ATPase activity with a Ki of 1.76 µM, displaying antitumor activity[1][2]. |
Animal study | While ML216 similarly inhibits the unwinding activity of the related BLM and WRN helicases in vitro, its biological effects in human cells predominantly rely on BLM, indicating a BLM-specific mechanism of action in vivo. An elucidating co-crystal structure of BLM bound to the inhibitor would be revealing. It's suggested that cellular conditions in vivo may prompt a WRN conformation resistant to ML216[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.04mL 2.61mL 1.30mL |
26.09mL 5.22mL 2.61mL |
CAS号 | 1430213-30-1 |
分子式 | C15H9F4N5OS |
分子量 | 383.32 |
SMILES Code | O=C(NC1=CC=C(F)C(C(F)(F)F)=C1)NC2=NN=C(S2)C3=CC=NC=C3 |
MDL No. | MFCD24849400 |
别名 | CID-49852229 |
运输 | 蓝冰 |
InChI Key | WMCOYUSJXXCHFH-UHFFFAOYSA-N |
Pubchem ID | 49852229 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |