ML216 Struktur

ML216

Bezeichnung:ML216

CAS-Nr1430213-30-1

Englisch Name:ML216

CBNumberCB02715652

SummenformelC15H9F4N5OS

Molgewicht383.32

MOL-Datei1430213-30-1.mol

ML216 physikalisch-chemischer Eigenschaften

Dichte	1.583±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO:29.0(Max Conc. mg/mL);75.65(Max Conc. mM)
pka	6.40±0.50(Predicted)
Aggregatzustand	powder
Farbe	light orange to dark orange

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

ML216 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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]
Verwenden
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.

ML216 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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