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.
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- CAS. Nr.: 1049742-84-8
- Formel: C11H13Cl3N2
- Molecular Weight:279.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
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.
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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. Nr. 1049742-84-8
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Molecular Weight 279.59
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Formel C11H13Cl3N2
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SMILES
ClC1=CC(NC(C)=C2CCN)=C2C(Cl)=C1.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DCAI hydrochloride Related Classifications
HY-118692A Related Classifications
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