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Merck
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SML1143

Sigma-Aldrich

PTC-209

≥98% (HPLC)

别名:

N-（2,6-二溴-4-甲氧基苯基）-4-（2-甲基咪唑并[1,2-a]嘧啶-3-基）-2-噻唑胺

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About This Item

经验公式（希尔记法）:
C17H13Br2N5OS
CAS号:
315704-66-6
分子量:
495.19
MDL號碼:
MFCD02110649
分類程式碼代碼:
12352200
PubChem物質ID:
329825677
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to brown

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

BrC1=CC(OC)=CC(Br)=C1NC2=NC(C3=C(C)N=C4N3C=CC=N4)=CS2

InChI

1S/C17H13Br2N5OS/c1-9-15(24-5-3-4-20-16(24)21-9)13-8-26-17(22-13)23-14-11(18)6-10(25-2)7-12(14)19/h3-8H,1-2H3,(H,22,23)

InChI 密鑰

XVOOCQSWCCRVDY-UHFFFAOYSA-N

應用

PTC-209已被用作B淋巴瘤Mo-MLV插入区1同源物（BMI1）抑制剂，用于研究其对以下方面的影响：
  • 犬骨肉瘤（OSA）细胞系的细胞活力
  • 卵巢癌（OvCa）细胞中脂质化的微管相关蛋白1轻链3（LC3B-II）和死骨片1（SQSTM1）蛋白的水平
  • 小鼠胚胎成纤维细胞（MEF）的心脏重编程效率

生化／生理作用

PTC-209 抑制癌基因 BMI-1（B 淋巴瘤 Mo-MLV 插入区 1 同源物）的表达，该基因编码参与细胞周期的多梳环 RING 指蛋白。 PTC-209 降低结肠直肠癌起始细胞（CIC）的自我更新特性。该化合物抑制肿瘤生长，并降低小鼠结肠癌肿瘤异种移植物中 CIC 的水平。

特點和優勢

该化合物是基因调控研究推荐产品。点击此处 ，查看更多基因调控精选产品。想要了解有关生物活性小分子在其他研究领域应用的更多信息，请访问 sigma.com/discover-bsm。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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Inhibition of BMI1 induces autophagy-mediated necroptosis
Dey A, et al.
Autophagy, 12(4), 659-670 (2016)
BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance
Shahi M H, et al.
PLoS ONE, 10(6), e0131006-e0131006 (2015)
Mohammad Alzrigat et al.
Oncotarget, 8(61), 103731-103743 (2017-12-22)
Multiple myeloma (MM) is a tumor of plasmablasts/plasma cells (PCs) characterized by the expansion of malignant PCs with complex genetic aberrations in the bone marrow (BM). Recent reports, by us and others, have highlighted the polycomb group (PcG) proteins as
Sami Al-Nadaf et al.
Veterinary and comparative oncology, 20(4), 871-880 (2022-07-15)
The BMI1 proto-oncogene, polycomb ring finger protein (BMI1) is a key component of the epigenetic polycomb repressor complex 1, and has been associated with aggressive behaviour and chemotherapeutic resistance in various malignances including human gliomas. Similar to humans, spontaneous canine
Junan Li et al.
Anticancer research, 40(1), 133-141 (2020-01-02)
Aberrant expression of the BMI1 oncogene has been prevalently found in a variety of human cancers, including cervical cancer. Recent studies have shown that PTC209, a specific BMI1 inhibitor, exhibits high potency in inhibiting the growth of colon, breast, oral
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