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

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.

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PAWI-2 Chemical Structure

PAWI-2 Chemical Structure

CAS No. : 1448427-02-8

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Description

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

 

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]
Molecular Weight

371.45

Formula

C19H21N3O3S

CAS No.
Appearance

Solid

Color

Brown to dark brown

SMILES

O=C1N(C2=CC=C(S(=O)(N3CCN(C)C4=C3C=CC=C4)=O)C=C2)CCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Purity & Documentation
References
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    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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PAWI-2
Cat. No.:
HY-123929
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