CBFβ Inhibitor (Synonyms: Core Binding Factor-β Inhibitor) |
Catalog No.GC15474
One-Click Copy Product Info
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CBFβ inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 493028-20-9
Sample solution is provided at 25 µL, 10mM.
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CBFβ inhibitor is a small molecule which binds to CBFβ and inhibits its association with Runx1 [1].
Core binding factors (CBFs) are heterodimeric transcription factors containing a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ. CBF dimers plays important roles in hematopoiesis and, when dysfunctional, in leukemia [2].The interaction of CBFβwith Runx2 has a critical role in bone development [3].
In vitro: The ELISA results have shown that CBFβ Inhibitor is very effective in inhibiting the CBFβ-Runx1 interaction with an IC50 of 3.2 μM. In the leukemia cell line ME-1 expressing CBFβ-SMMHC, CBFβ Inhibitor reduced cell proliferation dose-dependently. Treatment with CBFβ Inhibitor for 3 days showed an increase in apoptotic cells. Treatment with CBFβ Inhibitor for 14 days individually or with all-trans-retinoic acid (ATRA) resulted in cells with greater variation in size and shape, lower nuclear-to-cytoplasmic ratio, increased folding and lobation of nuclei, and more clumped chromatin. All of these morphology changes are consistent with differentiation to more mature forms. CBFβ Inhibitor at 50 μM increased proliferation of Hep-G2 cells. CBFβ treatment with Inhibitor resulted in a statistically significant reduction in Runx1 bound to DNA [1].
References:
[1]. Gorczynski M J, Grembecka J, Zhou Y, et al. Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFβ[J]. Chemistry & biology, 2007, 14(10): 1186-1197.
[2]. Swiers G, De Bruijn M, Speck N A. Hematopoietic stem cell emergence in the conceptus and the role of Runx1[J]. The International journal of developmental biology, 2010, 54: 1151.
[3]. Kundu M, Javed A, Jeon J P, et al. Cbfβ interacts with Runx2 and has a critical role in bone development[J]. Nature genetics, 2002, 32(4): 639-644.
| Cas No. | 493028-20-9 | SDF | |
| Synonyms | Core Binding Factor-β Inhibitor | ||
| Chemical Name | 5-ethyl-4-(4-methoxyphenyl)-2-thiazolamine | ||
| Canonical SMILES | COC1=CC=C(C2=C(CC)SC(N)=N2)C=C1 | ||
| Formula | C12H14N2OS | M.Wt | 234.3 |
| Solubility | ≤25mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.268 mL | 21.3402 mL | 42.6803 mL |
| 5 mM | 853.6 μL | 4.268 mL | 8.5361 mL |
| 10 mM | 426.8 μL | 2.134 mL | 4.268 mL |
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)