3031102-92-5
Chemical Structure
TRAP1-IN-2
- CAS No.: 3031102-92-5
- Formula:C46H42F6N2O5P2
- Molecular Weight:878.77
InChIKey: YBPGVKHPFGUNAS-UHFFFAOYSA-O
SMILES: O=C(C1=C(O)C=CC(C(N2CC(C(OC)=CC=C3)=C3C2)=O)=C1)N(C4)CC5=C4C=CC(OCCC[P+](C6=CC=CC=C6)(C7=CC=CC=C7)C8=CC=CC=C8)=C5.F[P-](F)(F)(F)(F)F
Biological Activity: TRAP1-IN-2 is a TRAP1-selective inhibitor, with a Kd value of 0.04 μM against human TRAP1. TRAP1-IN-2 exhibits more than 250-fold selectivity for Grp94 and shows no detectable affinity for cytosolic Hsp90α/β. TRAP1-IN-2 selectively induces the degradation of TRAP1 client proteins by inhibiting its ATPase activity, without triggering the heat shock response or affecting cytosolic Hsp90 client proteins. TRAP1-IN-2 suppresses oxidative phosphorylation, shifts cellular metabolism toward glycolysis, disrupts the stability of the TRAP1 tetramer and the mitochondrial membrane potential. TRAP1-IN-2 can be used in studies related to prostate cancer, cervical cancer, and ovarian cancer[1].
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TRAP1-IN-2 | TRAP1-IN-2 is a TRAP1-selective inhibitor, with a Kd value of 0.04 μM against human TRAP1. TRAP1-IN-2 exhibits more than 250-fold selectivity for Grp94 and shows no detectable affinity for cytosolic Hsp90α/β. TRAP1-IN-2 selectively induces the degradation of TRAP1 client proteins by inhibiting its ATPase activity, without triggering the heat shock response or affecting cytosolic Hsp90 client proteins. TRAP1-IN-2 suppresses oxidative phosphorylation, shifts cellular metabolism toward glycolysis, disrupts the stability of the TRAP1 tetramer and the mitochondrial membrane potential. TRAP1-IN-2 can be used in studies related to prostate cancer, cervical cancer, and ovarian cancer. | |||||||||||||||||||||
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