2. MAPK/ERK Pathway
  3. MEK
  4. Grb2 SH2 domain inhibitor 1

Grb2 SH2 domain inhibitor 1 is an inhibitor of the Grb2 SH2 domain with an IC50 of 0.40 μM. Grb2 SH2 domain inhibitor 1 is also a cell-permeable cyclic peptide that can enter the cytosol of mammalian cells. Grb2 SH2 domain inhibitor 1 downregulates the expression level of p-MEK. Grb2 SH2 domain inhibitor 1 can be used in the research of breast cancer.

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Grb2 SH2 domain inhibitor 1

Grb2 SH2 domain inhibitor 1 Chemical Structure

CAS No. : 3069455-54-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Grb2 SH2 domain inhibitor 1 Related Antibodies

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Description

Grb2 SH2 domain inhibitor 1 is an inhibitor of the Grb2 SH2 domain with an IC50 of 0.40 μM. Grb2 SH2 domain inhibitor 1 is also a cell-permeable cyclic peptide that can enter the cytosol of mammalian cells. Grb2 SH2 domain inhibitor 1 downregulates the expression level of p-MEK. Grb2 SH2 domain inhibitor 1 can be used in the research of breast cancer[1].

In Vitro

Grb2 SH2 domain inhibitor 1 (Compound 14) (5 μM; 2 h) exhibits a cytoplasmic entry efficiency of 49% in HeLa cells relative to CPP9 (HY-P10644), and enters HeLa cells via an endocytic mechanism[1].
Grb2 SH2 domain inhibitor 1 (0-30 μM; 2 h) dose-dependently inhibits the level of phosphorylated MEK in EGF-stimulated MDA-MB-468 cells, with an IC50 of approximately 15 μM[1].

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

Grb2 SH2 domain inhibitor 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-468 human breast cancer cells
Concentration: 0, 1, 5, 15, 30 μM
Incubation Time: 2 h
Result: Dose-dependently decreased the level of phosphorylated MEK (p-MEK) with an IC50 of ~15 μM.
Showed no effect on total MEK levels.
Exerted a less dramatic effect on ERK1/2 phosphorylation.
Molecular Weight

1463.58

Formula

C68H95N20O15P
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Cyclo(Tyr(PO3H2)-Arg-Arg-Pro-DPro-DArg-2Nal-Phe-Asn-Val)
Sequence Shortening

Cyclo(Tyr(PO3H2)-RRP-DPro-DArg-2Nal-FNV)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (17.08 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 0.6833 mL 3.4163 mL 6.8326 mL
5 mM 0.1367 mL 0.6833 mL 1.3665 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 0.6833 mL 3.4163 mL 6.8326 mL 17.0814 mL
5 mM 0.1367 mL 0.6833 mL 1.3665 mL 3.4163 mL
10 mM 0.0683 mL 0.3416 mL 0.6833 mL 1.7081 mL
15 mM 0.0456 mL 0.2278 mL 0.4555 mL 1.1388 mL
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Grb2 SH2 domain inhibitor 1 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:

Grb2 SH2 domain inhibitor 13069455-54-2MEKMitogen-activated protein kinase kinaseMAPKKMAP2KEGFdownstream signaling pathwaysHeLa cellsendosomes/lysosomesMDA-MB-468 cellsmammalian cellsbreast cancerphosphorylated MEKGrb2 SH2 domainphosphotyrosine-containing sequencesInhibitorinhibitorinhibit

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