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506384 BLM Helicase Inhibitor, ML216 - CAS 1430213-30-1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1430213-30-1C₁₅H₉F₄N₅OS

Products

Catalog NumberPackaging Qty/Pack
5.06384.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97 µM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 > 1.2 h) and plasma stability (~100% at 5 h).
Catalogue Number506384
Brand Family Calbiochem®
Synonyms1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216
References
ReferencesRosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.
Product Information
CAS number1430213-30-1
FormOrange solid
Hill FormulaC₁₅H₉F₄N₅OS
Chemical formulaC₁₅H₉F₄N₅OS
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetBLM
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.06384.0001 04055977243284

Documentation

BLM Helicase Inhibitor, ML216 - CAS 1430213-30-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Rosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision18-December-2013 JSW
Synonyms1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216
DescriptionA cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97 µM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 > 1.2 h) and plasma stability (~100% at 5 h).
FormOrange solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1430213-30-1
Chemical formulaC₁₅H₉F₄N₅OS
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesRosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol. 20, 55.