UC-857993

Cat. No.: HY-124514: FAQs
Data Sheet Handling Instructions

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UC-857993 is a selective SOS1-Ras inhibitor (K_d=14.7 μM, His₆-SOS1_cat), suppressing catalytic activity. UC-857993 also inhibits ERK and Ras activation, suppresses the growth of mouse embryonic fibroblasts (MEFs).

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

UC-857993 Chemical Structure

CAS No. : 487001-04-7

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K-Ras H-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
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Description

In Vitro

UC-857993 (0-80 μM; 3 d) specifically inhibits the growth of wild-type MEFs, but did not inhibit the growth of carcinogenic H-Ras(G12V) expressing MEF^[1].
UC-857993 (60 μM, 80 μM; 2 h) dose-dependently inhibits Ras activation and downstream ERK activation mediated through EGFR-SOS1-Ras-Raf1-MEK-ERK signaling^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	Mouse embryonic fibroblasts
Concentration:	0, 40, 60, and 80 μ M
Incubation Time:	3 days
Result:	Selectively inhibited the growth of mouse fibroblasts, as exerting inhibition against wild-type mouse embryonic fibroblasts but not mouse embryonic fibroblasts expressing carcinogenic H-Ras(G12V).

Western Blot Analysis^[1]

Cell Line:	NIH/3T3 cells
Concentration:	60 μM, 80 μM
Incubation Time:	2 hours; stimulated with 50 ng/ml EGF for 5 min
Result:	Inhibited EGF-induced the increase of the level of p-ERK and Ras-GTP.

Molecular Weight

403.90

Formula

C₂₅H₂₂ClNO₂

CAS No.

487001-04-7

SMILES

O=C(C1=CC2=C3N(C(C4=CC=CC=C4Cl)C5C2C=CC5)CC(CC=C6)C6C3=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Evelyn CR, et al. Combined rational design and a high throughput screening platform for identifying chemical inhibitors of a Ras-activating enzyme. J Biol Chem. 2015 May 15;290(20):12879-98. [Content Brief]

UC-857993 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

UC-857993487001-04-7UC857993UC 857993RasERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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