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Art. -Nr.: HY-145162

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SHP2-D26

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia.
(Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker).

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Reinheit: 95.83%
CAS. Nr.: 2458219-65-1
Formel: C₅₆H₇₉ClN₁₂O₆S₂
Molecular Weight:1115.89

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SHP2-D26 Chemical Structure

CAS. Nr.: 2458219-65-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia^[1]. (Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker).

IC₅₀ & Target

SHP2^[1]

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KYSE-520 cell line	IC₅₀	0.66 μM Compound: 26; SHP2-D26	Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay	[PMID: 32437146]
MV4-11	DC₅₀	2.6 nM Compound: 26; SHP2-D26	Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis	[PMID: 32437146]
MV4-11	IC₅₀	9.9 nM Compound: 26; SHP2-D26	Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay	[PMID: 32437146]

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.

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.

Chemical Information

CAS. Nr. 2458219-65-1
Appearance Solid
Molecular Weight 1115.89
Formel C₅₆H₇₉ClN₁₂O₆S₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Biol Chem

Bivalent target-binding bioPROTACs induce potent degradation of oncogenic SHP2. [Abstract]

2024 Jul 30:107616. PMID: 39089586

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8961 mL

4.4807 mL

8.9615 mL

5 mM

0.1792 mL

0.8961 mL

1.7923 mL

10 mM

0.0896 mL

0.4481 mL

0.8961 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein [published correction appears in J Med Chem. 2021 Jan 14;64(1):906-908]. J Med Chem. 2020;63(14):7510-7528. [Content Brief]

[2]. Wang M, et al. Correction to "Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein". J Med Chem. 2021 Jan 14;64(1):906-908. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SHP2-D26

1 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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SHP2-D26 purchased from MedChemExpress. Usage Cited in:

MedChemExpress Validation
KYSE-520 cells were seeded at 1*10⁶ cells/well in a 6-well plate and were cultured overnight. Then, cells were treated with 0-1000 nM SHP2-D26 (HY-145162) for 12 hours to assess the expression of SHP2. The results demonstrated that SHP2-D26 effectively degraded SHP2 protein. Primary antibody: SHP2 antibody (HY-P81898).

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SHP2-D26

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) SHP2-D26

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHP2-D26

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) SHP2-D26

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHP2-D26 Related Classifications

HY-145162 Related Classifications