SMDC818909
SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms.
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- CAS No.: 1147823-21-9
- 화학식: C14H13N5O
- 분자량:267.29
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
SMDC818909 binds to the D2 domain of full-length p97 with a Kd of 9.1 μM[1].
SMDC818909 (5-100 μM ATP) acts as a non-competitive inhibitor of p97 ATPase, with IC50 values of 26 μM, 11.5 μM and 4.9 μM under the conditions of 5, 20 and 100 μM ATP, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1147823-21-9
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분자량 267.29
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화학식 C14H13N5O
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SMILES
O=C(NC1=CC2=C(C=C1)NC(C)=C2)C3=NC=CN=C3N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)