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PAC-1

PAC-1 (Procaspase activating compound 1) 是一种 procaspase-3激活剂，诱导癌细胞凋亡，EC50为 2.08 μM，可用于研究淋巴瘤、黑色素瘤、实体瘤、乳腺癌和胸癌等治疗的试验。

CAS号

315183-21-2

分子式

C23H28N4O2

主要靶点

Autophagy|Apoptosis|Caspase

仅限科研使用

Cat No : CM03299

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Synonyms

Procaspase activating compound 1

验证数据展示

  • CAS No.: 315183-21-2

    PAC-1
    CAS#: 315183-21-2

产品信息

PAC-1 (Procaspase activating compound 1) has been used in trials studying the treatment of Lymphoma, Melanoma, Solid Tumors, Breast Cancer, and Thoracic Cancers, among others.

CAS号 315183-21-2
分子式 C23H28N4O2
主要靶点 Autophagy|Apoptosis|Caspase
主要通路 蛋白酶体|凋亡|自噬
分子量 392.49
纯度 99.77%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Procaspase activating compound 1

靶点活性

Procaspase-3:0.22 μM(EC50)

体内活性

PAC-1能够以延迟的方式诱导Bax/Bak双敲除细胞和Bcl-2和Bcl-xL过表达细胞中的细胞死亡,具有与野生型对应物相同的功效。PAC-1按caspase-3 非依赖性方式诱导细胞色素c释放,随后触发下游caspase-3激活和细胞死亡。PAC-1不能诱导Apaf-1敲除细胞中的细胞死亡和半胱天冬酶-3激活,这表明凋亡体形成对于通过PAC-1介导的细胞死亡的胱天蛋白酶-3激活是必需的。PAC-1诱导原发性癌细胞凋亡,IC50值为3 nM至1.41 μM,比邻近的非癌细胞更有效,IC50为5.02 μM至9.98 μM,这也与procaspase-3的浓度直接相关。PAC-1激活procaspase-3,产生caspase-3,EC50为 0.22 μM,且激活procaspase-7,EC50为 4.5 μM。癌细胞系中增高的caspase 3水平使 PAC-1 选择性诱导凋亡,按与procaspase-3 浓度成比例的方式,NCI-H226细胞的IC50为0.35 μM,UACC-62细胞的IC50为约3.5 μM。PAC-1通过螯合锌离子来激活胱天蛋白酶-3,从而减轻锌介导的抑制作用,并允许胱天蛋白酶原-3自身激活为胱天蛋白酶-3。

体外活性

PAC-1由于激活procaspase-3和随后诱导凋亡发挥体内抗肿瘤效果,与体外活性一致.用5 mg的稳定释放低剂量PAC-1处理小鼠,明显抑制ACHN肾移植瘤生长.用50或100 mg/kg PAC-1口服处理,明显剂量依赖性阻碍NCI-H226肺癌移植瘤生长,且明显阻止癌细胞浸润肺组织.

溶解度

1eq. HCl:29.4 mg/mL (75 mM),DMSO:39.3 mg/mL (100 mM)

细胞实验

Cells are exposed to various concentrations of PAC-1 for 72 hours. Cell death is quantified by the addition of MTS/PMS CellTiter 96 Cell Proliferation Assay reagent. The plates are incubated at 37 °C for approximately 1 hour (until the colored product formed), and the absorbance is measured at 490 n(Only for Reference)

参考文献

1.Putt KS, et al. Nat Chem Biol, 2006, 2(10), 543-550.
2.Peterson QP, et al. J Mol Biol, 2009, 388(1), 144-158.
3.Seervi M, et al. Cell Death Dis, 2011, 2, e207.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2