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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Apoptosis > MX-69CAS：1005264-47-0
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1005264-47-0 |
| Name | MX-69 |
| Molecular Formula | C27H26N2O4S |
| Molecular Weight | 474.57 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD24858136 |
| SMILES | O=C(O)C1=CC=C(C2C(CC=C3)C3C(C=C(S(=O)(NC4=CC(C)=C(C)C=C4)=O)C=C5)=C5N2)C=C1 |
| Target Point | MDM-2 |
| Passage | Apoptosis |
| Background | MX69 is an MDM2/XIAP inhibitor. |
| Biological Activity | MX69是MDM2/XIAP抑制剂，其结合MDM2 RING 蛋白的Kd值为2.34 μM。[1] |
| In Vitro | MX69以时间和剂量依赖性的方式抑制MDM2和XIAP的表达。在癌细胞中，MX69诱导内源性MDM2的泛素化。MX69通过诱导MDM2的自我泛素化和降解来下调MDM2。MDM2在对照组的EU-1细胞中的半衰期大于90分钟，而MX69的处理将降低MDM2的半衰期，MDM2的半衰期在MX69的处理下小于30分钟。在稳定转染了WT-MDM2或突变型MDM2-C464A的SK-N-SH细胞中，MX69显著地抑制WT-MDM2的表达、增加MDM2翻转、增强p53的半衰期，但对MDM2-C464A没有此影响。在MX69处理过的细胞中，p53被稳定下来并积累。MX69所介导的XIAP的抑制也是依赖于MDM2的。MX69激活caspases3，7，9以及促进PARP的分裂。MX69还可在ALL和NB细胞中发挥显著的细胞毒性作用，特别是过表达MDM2和WTp53的细胞中。MX69所诱导的细胞死亡主要是凋亡。MX69诱导的细胞凋亡和死亡作用依赖于MDM2、p53以及XIAP的表达。在体外，MX69对正常的人类骨髓的抑制作用很小[1]。 |
| In Vivo | 在体内实验中，MX69在表达MDM2的癌细胞中发挥其促凋亡、抗增殖的作用。MX69在动物中耐受良好，因为正常细胞/组织表达很少或不表达MDM2。100 mg/kg的MX69处理没有毒性作用。在正常细胞中，MX69对正常靶标(如p53的诱导)或脱靶信号通路没有激活效应。所以，特异性的MDM2抑制剂MX69可能是靶向治疗表达高水平MDM2的前列腺癌的非常有潜力的候选化合物[1]。 |
| Data Literature Source | [1] Gu L，et al. Cancer Cell. 2016，30(4):623-636. |
| Unit | Bottle |
| Specification | 5mg |
MX69是MDM2/XIAP抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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