1. Apoptosis Stem Cell/Wnt NF-κB
  2. MDM-2/p53 Wnt IKK Apoptosis Caspase
  3. PAWI-2

PAWI-2 是一种 p53 激活剂和 Wnt 抑制剂。PAWI-2 抑制不依赖 KRAS 的 β3-KRAS 信号传导。PAWI-2 选择性抑制 TBK1 的磷酸化。PAWI-2 激活细胞凋亡 (Apoptosis) (激活 caspase-3/7),并诱导 PARP 裂解。PAWI-2 促进视神经素转位进入细胞核并导致 G2/M 停滞。PAWI-2 逆转整合素 β3 KRAS 依赖性人类胰腺癌干细胞 (hPCSC) 的癌症干细胞特性,并克服耐药性。PAWI-2 抑制原位异种移植小鼠模型中 hPCSC 肿瘤的生长。

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PAWI-2 Chemical Structure

PAWI-2 Chemical Structure

CAS No. : 1448427-02-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model[1][2].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
10 nM
Compound: 19
Antiproliferative activity against human MCF7 cells after 24 hrs by SYBR green dye based fluorescence assay
Antiproliferative activity against human MCF7 cells after 24 hrs by SYBR green dye based fluorescence assay
[PMID: 30075999]
MCF7 EC50
13 nM
Compound: 19
Induction of apoptosis in human MCF7 cells after 24 hrs by caspase-Glo 3/7 reagent based luminescence assay
Induction of apoptosis in human MCF7 cells after 24 hrs by caspase-Glo 3/7 reagent based luminescence assay
[PMID: 30075999]
MDA-MB-231 IC50
13 nM
Compound: 19
Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by SYBR green dye based fluorescence assay
Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by SYBR green dye based fluorescence assay
[PMID: 30075999]
分子量

371.45

Formula

C19H21N3O3S

CAS 号
性状

固体

颜色

Brown to dark brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PAWI-2
目录号:
HY-123929
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