219506
CBFβ-Runx1 Inhibitor II
Synonym(s):
RUNX1/CBFβ inhibitor
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10 MG
$255.00
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10 MG
$255.00
About This Item
UNSPSC Code:
12352200
NACRES:
NA.28
Recommended Products
form
(Off-white solid)
Quality Level
storage condition
OK to freeze
solubility
soluble (DMSO (50 mg/ml))
storage temp.
2-8°C
Related Categories
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 Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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