2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. PCA-IN-1

PCA-IN-1 is a polyisoprenylated cysteinyl amide (PCA) inhibitor that acts on multiple KRAS mutant subtypes. PCA-IN-1 dissociates KRAS4B from its transport chaperones, prevents its localization to the plasma membrane, and blocks downstream oncogenic signaling pathways. PCA-IN-1 inhibits colony formation of KRAS-mutant lung cancer cells, induces sustained long-term growth inhibition, and suppresses cell migration. PCA-IN-1 is applicable to the research of KRAS-mutant lung cancer.

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

PCA-IN-1

PCA-IN-1 Chemical Structure

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PCA-IN-1 Related Antibodies

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Description

PCA-IN-1 is a polyisoprenylated cysteinyl amide (PCA) inhibitor that acts on multiple KRAS mutant subtypes. PCA-IN-1 dissociates KRAS4B from its transport chaperones, prevents its localization to the plasma membrane, and blocks downstream oncogenic signaling pathways. PCA-IN-1 inhibits colony formation of KRAS-mutant lung cancer cells, induces sustained long-term growth inhibition, and suppresses cell migration. PCA-IN-1 is applicable to the research of KRAS-mutant lung cancer[1].

IC50 & Target[1]

KRAS(G12C)

 

KRAS(G12A)

 

In Vitro

PCA-IN-1 (PCAIs) (3 μM; 12 days) exerts broad anti-tumor activity by inhibiting colony formation in NCI-H23 KRASG12C and NCI-H23 KRASG12A cells[1].
NSL-YHJ-2-27 potently inhibits the viability of NCI-H23 KRASG12C (IC50 = 3.0 μM) and NCI-H23 KRASG12A (IC50 = 3.2 μM) cells, with consistent efficacy across different mutants[1].
PCA-IN-1 (26 d) exerts broad and sustained long-term growth inhibitory effects on NCI-H23 KRASG12C and NCI-H23 KRASG12A cells[1].
PCA-IN-1 (3 d) significantly inhibits the migration of NCI-H23 KRASG12C and NCI-H23 KRASG12A cells, whereas Sotorasib (HY-114277) only inhibits the migration of cells carrying the KRASG12C mutant[1].
PCA-IN-1 alters the transcriptome profile of KRAS-mutant NCI-H23 cells, with the changes enriched in signal transduction, cell adhesion and cancer-related pathways[1].

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

PCA-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: NCI-H23 KRASG12C, NCI-H23 KRASG12A
Concentration: 3 μM
Incubation Time: 12 days
Result: Inhibited colony formation comparably to Sotorasib in NCI-H23 KRASG12C cells.
Showed significantly greater effectiveness in NCI-H23 KRASG12A cells than Sotorasib.
Molecular Weight

574.90

Formula

C33H58N4O2S
SMILES

C/C(C)=C\CC/C(C)=C/CC/C(C)=C/CSCC(C(NC1CCCCCCC1)=O)NC(CN2CCN(CC2)C)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PCA-IN-1 Related Classifications

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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:

PCA-IN-1RasNCI-H23 KRASG12Acancer-related pathwaysKRAS4BKRAS mutant subtypesoncogenic signalingNCI-H23 KRASG12Ctranscriptomic profilesplasma membraneKRAS-mutant lung cancer cellsInhibitorinhibitorinhibit

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