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AI-10-49

AI-10-49 is a selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM.

AI-10-49 Chemical Structure

AI-10-49 Chemical Structure

CAS: 1256094-72-0

Purity & Quality Control

Batch: Purity: 99.76%
99.76

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Biological Activity

Description AI-10-49 is a selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM.
Targets
CBFβ-SMMHC [1] CBFβ-SMMHC/RUNX1 [1]
(in FRET assay)
260 nM 0.26 μM
In vitro
In vitro AI-10-49 displays specific growth inhibition of inv(16)-positive cell line ME-1. AI-10-49 selectively binds to CBFβ-SMMHC, disrupts its binding to RUNX1, and restores RUNX1 transcriptional activity. [1]
Kinase Assay FRET assays
Cerulean-Runt domain is expressed and purified. Venus-CBFβ-SMMHC is constructed by inserting 6xHis tag and Venus into pET22b vector between NdeI and NcoI sites, and by inserting CBFβ-SMMHC (the CBFβ-SMMHC construct contains 369 amino acids, 1-166 from CBFβ and 166-369 from MYH11 (amino acids 1526-1730)) between the NcoI and BamHI sites. The fusion protein is purified by standard Ni-affinity chromatography with an on column benzonase treatment to remove residual DNA contaminants. Proteins are dialyzed into FRET buffer (25mM Tris-HCl, pH 7.5, 150mM KCl, 2mM MgCl2) prior to use. Protein concentrations are determined by UV absorbance of the Cerulean and Venus at 433 and 513 nm, respectively. Cerulean-Runt domain and Venus-CBFβ-SMMHC were mixed 1:1 to achieve a final concentration of 10 nM in 96 well black COSTAR plates. DMSO solutions of compounds are added to a final DMSO concentration of 5% (v/v) and the plates incubated at room temperature for one hour in the dark. A PHERAstar microplate reader is used to measure fluorescence (excitation at 433 nm and emission measured at 474 and 525 nm). For IC50 determinations, the ratios of the fluorescence intensities at 525 nm and 474 nm are plotted versus the log of compound concentration, and the resulting curve was fit to a sigmoidal curve using Origin7.0. Three independent measurements are performed and their average and deviation are used for IC50 data fitting.
Cell Research Cell lines HL-60, KG-1, THP-1, Kasumi-1, TUR 9, U937, and MOLM-13 cells
Concentrations ~10 μM
Incubation Time 48 hours
Method Cell lines are cultured in IMDM supplemented with 10%~20% fetal bovine serum (FBS) according to culture conditions indicated by ATCC and 1% penicillin/streptomycin (Pen/Strep). All cell lines are tested for mycoplasma. Cells are cultured at 300,000 cells per ml in 96 well plates for 24 and 48 hours in DMSO, or different of AI-10-47, AI-410-49, AI-4-57, or AI-4-88); each in duplicate or triplicate. Cell viability is evaluated using DAPI by flow cytometry. Data is analyzed using FlowJo software and Graphpad Prism software.
In Vivo
In vivo In mice transplanted with Cbfb+/MYH11;Nras+/G12D leukemic cells, AI-10-49 (200 mg/kg, i.p.) reduces leukemia expansion. [1]
Animal Research Animal Models Mice transplanted with Cbfb+/MYH11;Nras+/G12D leukemic cells
Dosages 200 mg/kg
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 660.52 Formula

C30H22F6N6O5
CAS No. 1256094-72-0 SDF Download AI-10-49 SDF
Smiles FC(F)(F)OC1=CC=C2[NH]C(=NC2=C1)C3=NC=C(OCCOCCOC4=CN=C(C=C4)C5=NC6=C([NH]5)C=CC(=C6)OC(F)(F)F)C=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (93.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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