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5.06384

BLM Helicase Inhibitor, ML216

Name: BLM Helicase Inhibitor, ML216
Brand: MM

Synonym(s):

BLM Helicase Inhibitor, ML216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216, ML-216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₉F₄N₅OS

CAS Number:

1430213-30-1

Molecular Weight:

383.32

MDL number:

MFCD24849400

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥97% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

assay

≥97% (HPLC)

Quality Segment

100

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

orange

solubility

DMSO: 10 mg/mL

storage temp.

2-8°C

SMILES string

FC(F)(F)c1c(ccc(c1)NC(=O)Nc2[s]c(nn2)c3ccncc3)F

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)

InChI key

WMCOYUSJXXCHFH-UHFFFAOYSA-N

Description

General description

A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM^636-1298 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 (T_1/2 >1.2 h) and plasma stability (~100% at 5 h).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
BLM

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c