2. Protein Tyrosine Kinase/RTK PROTAC Metabolic Enzyme/Protease
  3. SHP2 PROTACs Phosphatase
  4. SHP2-D26

SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent.

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SHP2-D26 Chemical Structure

SHP2-D26 Chemical Structure

CAS No. : 2458219-65-1

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Based on 1 publication(s) in Google Scholar

SHP2-D26 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent[1].

IC50 & Target

SHP2[1]
In Vitro

SHP2-D26 (0, 3, 10, 30, 100, 300 nM; 12 hours) effectively reduces SHP2 protein in a dosedependent manner, with DC50 values of 6.0 nM, 2.6 nM in KYSE520 and MV-4-11 cells, respectively[1].
SHP2-D26 (100 nM; 0, 2, 4, 8, 12, 24 hours) reduces the SHP2 protein level within 4 h and completes SHP2 depletion with 8 h in KYSE520 and MV-4-11 cells[1].
SHP2-D26 (0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells; 4 days) achieves IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively[1].

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

SHP2-D26 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells
Incubation Time: 4 days
Result: Achieved IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 12 hours
Result: Reduced SHP2 protein in a dosedependent manner, with DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 100 nM
Incubation Time: 0, 2, 4, 8, 12, 24 hours
Result: Reduced the SHP2 protein level within 4 h and completed SHP2 depletion with 8 h.
Molecular Weight

1115.89

Formula

C56H79ClN12O6S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC(C(SC1=NC=C(N2CCC(N)(CC2)C)N=C1N)=CC=C3)=C3NC(CCC(N(CC4)CCN4CCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O)=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 : 83.33 mg/mL (74.68 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 0.8961 mL 4.4807 mL 8.9615 mL
5 mM 0.1792 mL 0.8961 mL 1.7923 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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 0.8961 mL 4.4807 mL 8.9615 mL 22.4036 mL
5 mM 0.1792 mL 0.8961 mL 1.7923 mL 4.4807 mL
10 mM 0.0896 mL 0.4481 mL 0.8961 mL 2.2404 mL
15 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4936 mL
20 mM 0.0448 mL 0.2240 mL 0.4481 mL 1.1202 mL
25 mM 0.0358 mL 0.1792 mL 0.3585 mL 0.8961 mL
30 mM 0.0299 mL 0.1494 mL 0.2987 mL 0.7468 mL
40 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5601 mL
50 mM 0.0179 mL 0.0896 mL 0.1792 mL 0.4481 mL
60 mM 0.0149 mL 0.0747 mL 0.1494 mL 0.3734 mL
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SHP2-D26 Related Classifications

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.

Keywords:

SHP2-D262458219-65-1SHP2PROTACsPhosphataseSrc homology phosphatase 2PTPN11KYSE520 cellsMV-4-11 cellscancerneddylation-dependentproteasome-dependentInhibitorinhibitorinhibit

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