1. Protein Tyrosine Kinase/RTK PROTAC Metabolic Enzyme/Protease Apoptosis
  2. SHP2 PROTACs Phosphatase Apoptosis
  3. SHP2 protein degrader-1

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases.

For research use only. We do not sell to patients.

SHP2 protein degrader-1 Chemical Structure

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

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5 mg USD 1215 In-stock
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Description

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]

In Vitro

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

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

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.
Molecular Weight

908.83

Formula

C42H51Cl2N11O8

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCOCCN4N=NC(CNC5(CCN(CC5)C6=CN=C(C7=C(Cl)C(Cl)=CC=C7)C(N)=N6)C)=C4)=CC=C3)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (121.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1003 mL 5.5016 mL 11.0032 mL
5 mM 0.2201 mL 1.1003 mL 2.2006 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1003 mL 5.5016 mL 11.0032 mL 27.5079 mL
5 mM 0.2201 mL 1.1003 mL 2.2006 mL 5.5016 mL
10 mM 0.1100 mL 0.5502 mL 1.1003 mL 2.7508 mL
15 mM 0.0734 mL 0.3668 mL 0.7335 mL 1.8339 mL
20 mM 0.0550 mL 0.2751 mL 0.5502 mL 1.3754 mL
25 mM 0.0440 mL 0.2201 mL 0.4401 mL 1.1003 mL
30 mM 0.0367 mL 0.1834 mL 0.3668 mL 0.9169 mL
40 mM 0.0275 mL 0.1375 mL 0.2751 mL 0.6877 mL
50 mM 0.0220 mL 0.1100 mL 0.2201 mL 0.5502 mL
60 mM 0.0183 mL 0.0917 mL 0.1834 mL 0.4585 mL
80 mM 0.0138 mL 0.0688 mL 0.1375 mL 0.3438 mL
100 mM 0.0110 mL 0.0550 mL 0.1100 mL 0.2751 mL
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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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Product Name:
SHP2 protein degrader-1
Cat. No.:
HY-145159
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