ML216
ML216
CAS: 1430213-30-1
Molecular Formula: C15H9F4N5OS
ML216 - Names and Identifiers
ML216 - Physico-chemical Properties
| Molecular Formula | C15H9F4N5OS |
| Molar Mass | 383.32 |
| Density | 1.583±0.06 g/cm3(Predicted) |
| Solubility | DMSO: 1.71 mg/mL |
| Appearance | powder |
| Color | light orange to dark orange |
| pKa | 6.40±0.50(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 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. |
| In vivo study | 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. |
ML216 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
ML216 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.609 ml | 13.044 ml | 26.088 ml |
| 5 mM | 0.522 ml | 2.609 ml | 5.218 ml |
| 10 mM | 0.261 ml | 1.304 ml | 2.609 ml |
| 5 mM | 0.052 ml | 0.261 ml | 0.522 ml |
Last Update：2024-01-02 23:10:35
ML216 - Reference Information
| biological activity | ML216 (CID-49852229) is an effective, selective, and anti-tumor activity Inhibitor of DNA unwinding activity of BLM(Bloom's syndrome protein). The IC50 values of ML216 inhibiting helicase BLM636-1298 and BLMfull-length are 0.97 μM and 2.98 μM respectively. |
| target | TargetValue BLM 636-1298 (Cell-free say) 0.97 μM BLM full-length (Cell-free say) 2.98 μM |
| Target | Value |
| BLM 636-1298 (Cell-free assay) | 0.97 μM |
| BLM full-length (Cell-free assay) | <2.98 μM |
| in vitro study | 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 led 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 μ m) and a truncated WRN 500-946 ( IC 50 of 12.6 μ m), 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. |
| 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 banner. |
| in vivo research | 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 made it resistant to ML216. |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: CID-49852229 Visit Supplier Webpage Request for quotationCAS: 1430213-30-1
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: ML216 Visit Supplier Webpage Request for quotationCAS: 1430213-30-1
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: ML216 Visit Supplier Webpage Request for quotationCAS: 1430213-30-1
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: ML216 Visit Supplier Webpage Request for quotationCAS: 1430213-30-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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