1. Autophagy PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  2. AUTACs SHP2 Apoptosis Autophagy Atg8/LC3
  3. SHP2 protein degrader-3

SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC50 = 3.22 μM) and anti-tumor activity (IC50 = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834)).

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SHP2 protein degrader-3 Chemical Structure

SHP2 protein degrader-3 Chemical Structure

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Description

SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC50 = 3.22 μM) and anti-tumor activity (IC50 = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834))[1].

In Vitro

SHP2 protein degrader-3 (Compound SA-8) (24-72 h) exhibits anti-proliferative activity against HeLa cells, with IC50s of 5.59 μM (24 h), 4.25 μM (48 h) and 4.81 μM (72 h)[1]. SHP2 protein degrader-3 (0-10 μM, 24-96 h) degrades SHP2 in a time- and dose-dependent manner in HeLa cells, with a DC50 of 3.22 μM and Dmax of 80.47%[1]. SHP2 protein degrader-3 (10 μM, 72 h) induces SHP2 degradation via autophagy-lysosome pathway[1]. SHP2 protein degrader-3 (1.1-30 μM, 72 h) induces apoptosis at different concentrations in cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Blocked SHP2 degradation when Pre-treatment with GW5074 (HY-10542) (1 μM) or SHP099 (HY-100388) (1 μM) for 4 h.
Blocked SHP2 degradation when Pre-treatment with Chloroquine (HY-17589A) (1 μM) or 3-Methyladenine (3-MA) (HY-19312) (0.125 nM/1 μM) for 4 h.
Blocked SHP2 degradation when Pre-treatment with MG132 (HY-13259) (50 nM) for 4 h.
Enhanced SHP2 degradation when Pre-treatment with Rapamycin (HY-10219) (6 μM) for 4 h.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0.12, 0.37, 1.1, 3.3, 10 μM
Incubation Time: 48 h
Result: Increased the LC3 levels in HeLa cells.

Apoptosis Analysis[1]

Cell Line: HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells
Concentration: 1.1, 3.3, 10, 20, 30 μM
Incubation Time: 72 h
Result: Induced apoptosis at different concentrations in HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells.
Molecular Weight

1213.58

Formula

C46H51Br2Cl2IN10O7

SMILES

CC1(CCN(CC1)C2=CN=C(C(N)=N2)C3=CC=CC(Cl)=C3Cl)NCC4=CN(CCOCCOCCOCCOCCNC(COC5=C(C=C(C=C5Br)/C=C6C(NC7=C\6C=C(C=C7)I)=O)Br)=O)N=N4

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Please store the product under the recommended conditions in the Certificate of Analysis.

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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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Product Name:
SHP2 protein degrader-3
Cat. No.:
HY-175204
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