DCAI hydrochloride
DCAI hydrochloride is a KRas inhibitor with a Kd value of 1.1 mM. DCAI hydrochloride directly binds to the Ras protein and competitively inhibits SOS-mediated nucleotide release (IC50 = 155 μM) and exchange reaction (IC50 = 342 μM). DCAI hydrochloride binds to the pocket at the Ras-SOS interface and blocks the formation of the Ras-SOS complex intermediate by impeding salt bridge formation through steric hindrance and the induction of Ras conformational changes. DCAI hydrochloride is used in the study of wild-type and mutant Ras tumors.
For research use only. We do not sell to patients.
- CAS No.: 1049742-84-8
- Formula: C11H13Cl3N2
- Molecular Weight:279.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
K-RAS 1.1 mM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
15.8 μM
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Inhibition of Venus-RBD-CRD membrane recruitment (a marker of Ras-GTP levels) in human HEK-293T cells assessed via live-cell imaging.
Inhibition of Venus-RBD-CRD membrane recruitment (a marker of Ras-GTP levels) in human HEK-293T cells assessed via live-cell imaging.
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17392120 |
In Vitro
DCAI (pre-incubation for 5 min; detection duration of 30 min) hydrochloride potently inhibits SOScat-catalyzed guanine nucleotide exchange of purified KRasGDP protein, with a mean IC50 of 342 μM.
DCAI (25 μM) hydrochloride does not affect the localization of full-length Ras at the cell membrane, nor does it cause widespread disruption of plasma membrane protein interactions in HEK-293T cells[2].
DCAI hydrochloride (100 μM; 2 h) reduces EGF (HY-P7109)-stimulated endogenous RasGTP levels in HEK 293T cells[2].
DCAI hydrochloride blocks the plasma membrane aggregation of fluorescent probes containing the cRaf RBD-CRD domain in HEK-293T cells (EC50 = 15.8 μM) and inhibits endogenous Ras activation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK-293T
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Concentration:100 μM
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Incubation Time:treatment for 2 hours followed by EGF stimulation for 5 minutes
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Result:Attenuated the Ras activation induced by EGF stimulation.
Chemical Information
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CAS No. 1049742-84-8
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Molecular Weight 279.59
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Formula C11H13Cl3N2
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SMILES
ClC1=CC(NC(C)=C2CCN)=C2C(Cl)=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DCAI hydrochloride Related Classifications
HY-118692A Related Classifications
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