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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > ApabetaloneCAS：1044870-39-4
Molecular Formula：C20H22N2O5
Molecular Weight：370.4
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to yellow Solid
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| CAS | 1044870-39-4 |
| Name | Apabetalone |
| Molecular Formula | C20H22N2O5 |
| Molecular Weight | 370.4 |
| Solubility | Soluble in DMSO ≥3mg/mL |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18633270 |
| SMILES | COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1 |
| Target Point | Epigenetic Reader Domain（BD2） |
| Passage | Epigenetics |
| Background | Apabetalone is a potent BET bromodomain inhibitor that acts on BD2. |
| Biological Activity | Apabetalone (RVX-208) 是一种 BET 转录抑制剂，作用于 BD1 和 BD2，IC50 分别为 87±10 μM 和 0.51±0.041 μM。[1-3] |
| IC50 | 510±41nM(BD2)，87±10μM(BD1)[1] |
| Data Literature Source | [1]. Picaud S，et al. RVX-208，an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. [2]. McLure KG，et al. RVX-208，an inducer of ApoA-I in humans，is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. [3]. Jahagirdar R，et al. A novel BET bromodomain inhibitor，RVX-208，shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236(1):91-100 |
| Unit | Bottle |
| Specification | 5mg 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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