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GANT 61

GANT 61 (GANT61) 是一种Gli1和Gli2抑制剂，靶向Hedgehog/GLi 通路。

CAS号

500579-04-4

分子式

C27H35N5

主要靶点

Autophagy|Hedgehog/Smoothened

仅限科研使用

Cat No : CM04230

Print datasheet

Synonyms

GANT61|NSC 136476

验证数据展示

  • CAS No.: 500579-04-4

    GANT 61
    CAS#: 500579-04-4

产品信息

GANT 61 is an inhibitor for Gli1 and Gli2.

CAS号 500579-04-4
分子式 C27H35N5
主要靶点 Autophagy|Hedgehog/Smoothened
主要通路 自噬|G蛋白偶联受体|干细胞
分子量 429.6
纯度 98.31%， 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 GANT61|NSC 136476

靶点活性

GLI1:5 μM

体内活性

GANT61以GLI依赖性方式有效抑制体外肿瘤细胞增殖。30 μM GANT61导致急性髓系白血病细胞生长停滞和凋亡。GANT61对人结肠癌细胞系具有强大的细胞毒性,且消除集落生成。GANT61作用于慢性淋巴细胞性白血病细胞,而非正常的B淋巴细胞,诱导细胞凋亡。GANT61在人结肠癌细胞系的早期S期中诱导DNA复制的抑制,导致ATM-Chk2轴的DNA损伤信号传导和诱导细胞死亡。GANT61抑制GLI1的DNA结合能力。GANT61抑制hedgehog信号,IC50为5 μM,比作用于其他通路选择性高（如TNF信号/NFκB激活,糖皮质激素受体基因转录,及Ras-Raf-Mek-Mapk级联）。

体外活性

携带SK-N-AS神经母细胞瘤移植瘤的裸鼠口服饲喂50 mg/kg GANT61,在实验第12天明显抑制肿瘤生长,与对照组相比,肿瘤体积减少63％.在注射GLI1阳性22Rv1前列腺癌细胞的裸鼠中,GANT61诱导肿瘤生长退化,直到观察不到明显的肿瘤.

溶解度

Ethanol:43 mg/mL (100 mM),DMSO:21.5 mg/mL (50 mM)

细胞实验

BrdU Incorporation Assay. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96-well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed.(Only for Reference)

参考文献

1.Lauth M, et al. Proc Natl Acad Sci, 2007, 104(20), 8455-8560
2.Desch P, et al. Oncogene, 2010, 29(35), 4885-4895.
3.Mazumdar Y, et al. Cancer Res, 2011, 71(3), 1092-1102.
4.Mazumdar T, et al. Cancer Res, 2011,71(17), 5904-5914.
5.Pan D, et al. Leuk Res, 2012, 36(6), 742-748.
6.Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone[J]. Journal of Endocrinology. 2020, 244(1): 177-187.

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