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MilliporeSigma

219506

Sigma-Aldrich

CBFβ-Runx1 Inhibitor II

Synonym(s):

CBFβ-Runx1 Inhibitor II, RUNX1/CBFβ inhibitor

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About This Item

Linear Formula:
C13H10ClN3O
CAS Number:
UNSPSC Code:
12352200
NACRES:
NA.28

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form

(Off-white solid)

Quality Level

storage condition

OK to freeze

solubility

soluble (DMSO (50 mg/ml))

storage temp.

2-8°C

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This Item
681641553511119114
Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

General description

A cell-permeable benzodiazepine that suppresses CBFα/Runx1-CBFβ transactivation activity (by 42% in 293-0 cell-based reporter assay; [Ro5-3335] = 25 µM) via direct affinity bindings to both subunits of the heterodimeric transcription factor complex. Shown to inhibit oncogenic fusion CBFB-MYH11-, TEL-RUNX1-, and RUNX1-ETO-, dependent leukemia cells proliferation (IC50 = 1.1, 17.3, and 21.7 µM, respectively, in ME-1, REH, and Kasumi-1 cultures) in vitro and more effectively reduce peripheral blood c-kit+ population (300 mg/kg/d via animal feed on days 10 to 40 after transplant) than Cytarabine (Cat. No. 251010; 100 mg/kg/d via i.p. on days 10 to 14 after transplant) in a murine Cbfb-MYH11 leukemia transplant model (49%, 17.5%, and <1% c-kit+ cells, respectively, 21 days after transplant in saline, Cytarabine, and Ro5-3335 treatment group) in vivo. Comparing to CBFβ-Runx1 Inhibitor I (Cat. No. 219505), Ro5-3335 modulates the Runx1-CBFβ heterodimer formation without completely disrupting the subunits interaction.

Application

The CBFΒ-Runx1 Inhibitor II, Ro5-3335, also referenced under CAS 30195-30-3, suppresses CBFΑ/Runx1-CBFΒ transactivation activity (25 µM; 293-0 cells) via direct bindings to both subunits of the heterodimeric transcription factor complex.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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