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CB-5083

CB-5083

Catalog Number:
L002371392APE
Mfr. No.:
APE-B6032
Price:
$188
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      • Overview

        • Please contact us at for specific academic pricing.

          Background

          IC50: 15.4 nM
          CB-5083 is an orally bioavailable inhibitor of p97. P97 is an AAA-ATPase involved in multiple cellular functions such as organelle membrane homotypic fusion and sorting of endosomal cargo. P97 is also known as valosin-containing protein which plays important roles in regulating protein homeostasis [1].
          In vitro: CB-5083 is a selective potent inhibitor of p97’s second ATPase domain. CB-5083 might compete with ATP for the same binding site but may adopt a different orientation[2]. The IC50 of CB-5083 against wild-type (WT) p97 was 15.4 nM. CB-5083 could dose-dependently increase the cytosolic protein degradation in HEK293T, A549 and HCT116 cell lines [1]. CB-5083 treatment (2.5 μM) of A549 cells for 24h could induce cancer cell death [1].
          In vivo: In female nude mice bearing HCT116, A549 lung carcinoma, and AMO-1 multiple myeloma xenograft tumors, oral administration of CB-5083 (100 mg/kg) for 6 h showed a significant antitumor response in tumors (TGI = 63%, p < 0.0001) [1,2].
          Clinical trial: CB-5083 has entered phase 1 clinical trials in patients with multiple myeloma and solid tumors.

          Anderson D J, Le Moigne R, Djakovic S, et al. Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis[J]. Cancer cell, 2015, 28(5): 653-665.
          Zhou H J, Wang J, Yao B, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)[J]. Journal of medicinal chemistry, 2015, 58(24): 9480-9497.

      • Properties
        • Alternative Name
          1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide
          CAS Number
          1542705-92-9
          Molecular Formula
          C24H23N5O2
          Molecular Weight
          413.47
          Appearance
          A solid
          Purity
          98.03%
          Solubility
          insoluble in H2O; ≥20.65 mg/mL in DMSO; ≥4.4 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Josephine Bock, Nathalie K€uhnle, et al. "Rhomboid protease RHBDL4 promotes retrotranslocation of aggregation-prone proteins for degradation." Cell Rep. 2022 Aug 9;40(6):111175. PMID: 35947953
          2. Chi-Wei Yeh, Wei-Chieh Huang, et al. "The C-degron pathway eliminates mislocalized proteins and products of deubiquitinating enzymes." EMBO J. 2021 Apr 1;40(7):e105846. PMID: 33469951
          3. Zhang H, Read C, et al. "The Human Cytomegalovirus Nonstructural Glycoprotein UL148 Reorganizes the Endoplasmic Reticulum." mBio. 2019 Dec 10;10(6). pii: e02110-19. PMID: 31822584
          4. Nathalie Kühnle, Josephine Bock, et al. "Intramembrane protease RHBDL4 interacts with erlin complex to target unstable soluble proteins for degradation." bioRxiv. 2019 November 20.

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