1. GPCR/G Protein
  2. Ras
  3. SAH-SOS1A

SAH-SOS1A 

Cat. No.: HY-P2265
Handling Instructions

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.

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

Custom Peptide Synthesis

SAH-SOS1A Chemical Structure

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

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Description

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS[1].

IC50 & Target[1]

KRAS-SOS1

 

KRas G12C

140 nM (EC50)

KRas G12D

109 nM (EC50)

KRas G12V

154 nM (EC50)

KRas G12S

155 nM (EC50)

KRas Q61H

175 nM (EC50)

K-Ras WT

106 nM (EC50)

In Vitro

SAH-SOS1A (0.625-40 μM) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected[1].
SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation[1].

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

Cell Viability Assay[1]

Cell Line: Panc 10.05 cells bearing the KRAS G12D mutation
Concentration: 0.625-40 μM
Incubation Time: 24 hours
Result: Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis[1]

Cell Line: Panc 10.05 cells
Concentration: 5-40 μM
Incubation Time: Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result: Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.
In Vivo

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2[1].

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

Molecular Weight

2187.53

Formula

C₁₀₀H₁₅₉N₂₇O₂₈

CAS No.
Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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