UMB-32 |
| カタログ番号GC14168 |
強力な選択的 BRD4 阻害剤である UMB-32 は、550 nM の Kd と 637 nM の IC50 で BRD4 に結合します。 UMB-32 は、ブロモドメインを含む転写因子である TAF1 に対しても効力を示します。
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Cas No.: 1635437-39-6
Sample solution is provided at 25 µL, 10mM.
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UMB-32 is a potent, selective inhibitor of the BET bromodomain BRD4 [1]. The BET family (BRD2, BRD3, BRD4, and BRDT) functions as transcriptional coactivator proteins. BET bromodomains are also important mediators of cell cycle progression and facilitate developmental transitions such as spermiogenesis. Deregulation of BET bromodomain function has been observed in numerous malignancies. BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer [1].
In vitro: UMB-32 bound to BRD4 with a Kd value of 550 nM and 724 nM cellular potency in BRD4-dependent lines. UMB-32 showed potency against TAF1, a bromodomain-containing transcription factor. UMB-32 showed markedly increased potency for the BET proteins associated with a dramatic improvement in selectivity. UMB-32 potently bound to the TAF1 and TAF1L with the Kd values of 560nM and 1.3 μM, respectively [1].
Reference:
[1] McKeown M R, Shaw D L, Fu H, et al. Biased multicomponent reactions to develop novel bromodomain inhibitors[J]. Journal of medicinal chemistry, 2014, 57(21): 9019-9027.
| Cas No. | 1635437-39-6 | SDF | |
| Chemical Name | N-(1,1-dimethylethyl)-2-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-imidazo[1,2-a]pyrazin-3-amine | ||
| Canonical SMILES | CC(C)(C)NC1=C(N=C2N1C=CN=C2)C3=CC=C(C4=C(C)ON=C4C)C=C3 | ||
| Formula | C21H23N5O | M.Wt | 361.4 |
| 溶解度 | ≤20mg/ml in ethanol;10mg/ml in DMSO;20mg/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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.767 mL | 13.8351 mL | 27.6702 mL |
| 5 mM | 0.5534 mL | 2.767 mL | 5.534 mL |
| 10 mM | 0.2767 mL | 1.3835 mL | 2.767 mL |
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- Purity: >98.00%
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