ML216
- CAS No.
- 1430213-30-1
- Chemical Name:
- ML216
- Synonyms
- ML216;CS-1561;CID49852229;CID-49852229;CID 49852229;ML216 (ML 216;ML216(CID4985229);ML216(CID-49852229);ML216, 10 mM in DMSO;BLM Helicase Inhibitor, ML216
- CBNumber:
- CB02715652
- Molecular Formula:
- C15H9F4N5OS
- Molecular Weight:
- 383.32
- MDL Number:
- MFCD24849400
- MOL File:
- 1430213-30-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| ML216 ≥98% (HPLC) | SML0661 | 5MG | $98.5 |
| ML216 ≥98% (HPLC) | SML0661 | 25MG | $397 |
| ML-216 ≥98% | 15186 | 1mg | $36 |
| ML-216 ≥98% | 15186 | 5mg | $75 |
| ML-216 ≥98% | 15186 | 10mg | $132 |
| More product size | |||
| Density | 1.583±0.06 g/cm3(Predicted) |
|---|---|
| storage temp. | 2-8°C |
| solubility | DMSO:29.0(Max Conc. mg/mL);75.65(Max Conc. mM) |
| form | powder |
| pka | 6.40±0.50(Predicted) |
| color | light orange to dark orange |
| InChI | 1S/C15H9F4N5OS/c16-11-2-1-9(7-10(11)15(17,18)19)21-13(25)22-14-24-23-12(26-14)8-3-5-20-6-4-8/h1-7H,(H2,21,22,24,25) |
| InChIKey | WMCOYUSJXXCHFH-UHFFFAOYSA-N |
| SMILES | FC(F)(F)c1c(ccc(c1)NC(=O)Nc2[s]c(nn2)c3ccncc3)F |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
ML216 price More Price(38)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0661 | ML216 ≥98% (HPLC) | 1430213-30-1 | 5MG | $98.5 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML0661 | ML216 ≥98% (HPLC) | 1430213-30-1 | 25MG | $397 | 2026-04-30 | Buy |
| Cayman Chemical | 15186 | ML-216 ≥98% | 1430213-30-1 | 1mg | $36 | 2026-04-30 | Buy |
| Cayman Chemical | 15186 | ML-216 ≥98% | 1430213-30-1 | 5mg | $75 | 2026-04-30 | Buy |
| Cayman Chemical | 15186 | ML-216 ≥98% | 1430213-30-1 | 10mg | $132 | 2026-04-30 | Buy |
ML216 Chemical Properties,Uses,Production
Description
Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-
Uses
Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM). At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.[Cayman Chemical]
Uses
ML216 has been used in cell proliferation assays.
Definition
ChEBI: 1-[4-fluoro-3-(trifluoromethyl)phenyl]-3-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)urea is a member of ureas.
Biochem/physiol Actions
ML216 is a membrane permeable selective inhibitor of Bloom (BLM) helicase, a member of the RecQ DNA helicase family. Bloom′s syndrome, caused by a mutation in BLM, is associated with susceptibility to cancer, growth retardation, immunodeficiency, sunlight sensitivity, and fertility defects. ML216 is selective for BLM over other members of the RecQ family, especially in vivo, and appears to act at the BLM-nucleic acid substrate binding site, inhibiting DNA binding and blocking BLM′s helicase activity. ML216 could be useful in studies of tumor cells depending on the ALT (alternative lengthening of telomeres) mechanism for telomere maintenance rather than on telomerase, which are proposed to be susceptible to BLM inhibition.
in vivo
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[2].
References
[1] GIANG HUONG NGUYEN. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells.[J]. Chemistry & biology, 2013, 20 1: 55-62. DOI: 10.1016/j.chembiol.2012.10.016
ML216 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32998 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6290 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6378 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 38999 | 58 |
| Chemtour Biotech Co., Ltd | market@chemtour.com | China | 1517 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11674 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +86-18327326525 | masar@topule.com | China | 8433 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57473 | 58 | |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +86-0086-13720134139 | orders@jknbiochem.com | China | 5215 | 58 |
