Oprozomib (ONX-0912)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    ONX-0912 (as known as oprozomib), discovered during a medicinal chemistry effort using tripeptide epoxyketones, is an orally bio-available and potent proteasome inhibitor that inhibits growth and induces apoptosis in bortezomib resistant multiple myeloma (MM) cells. Although ONX-0912, an analog of carfilzomib, is structurally distinct from bortezomib, it possesses the same ability as bortezomib to predominantly inhibit chymotrypsin-like activity of the proteasome. ONX-0912 exhibits significant anti-MM activities to reduce tumor progression and prolong survival in many animal tumor model studies, which are associated with activation of caspase-3, caspase-8, caspase-9, and poly(ADP) ribose polymerase and inhibition of anglogensis and MM cells migration.
- Properties
  - Alternative Name
    
    ONX-0912,ONX0912,ONX 0912,PR 047,Oprozomib; N-[(2S)-3-methoxy-1-[[(2S)-3-methoxy-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide
    
    CAS Number
    
    935888-69-0
    
    Molecular Formula
    
    C25H32N4O7S
    
    Molecular Weight
    
    532.61
    
    Appearance
    
    A solid
    
    Purity
    
    99.13%
    
    Solubility
    
    ≥26.6 mg/mL in DMSO; insoluble in H2O; ≥2.77 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. T. Ukmar-Godec, P. Fang, et al. "Proteasomal degradation of the intrinsically disordered protein tau at single-residue resolution." Sci Adv. 2020 Jul 22;6(30):eaba3916. PMID:32832664
    2. Felix Lambrecht. "Computational methods for the structure determination of highly dynamic molecular machines by cryo-EM." Georg-August-Universit?t G?ttingen. 2019.
    3. McCourt JL, Talsness DM, et al. "Mouse models of two missense mutations in actin-binding domain 1 of dystrophin associated with Duchenne or Becker muscular dystrophy." Hum Mol Genet. 2018 Feb 1;27(3):451-462. PMID:29194514
    4. Haselbach D, Schrader J, et al. "Long-range allosteric regulation of the human 26S proteasome by 20S proteasome-targeting cancer drugs." Nat Commun. 2017 May 25;8:15578. PMID:28541292
    5. Schrader J, Henneberg F, et al. "The inhibition mechanism of human 20S proteasomes enables next-generation inhibitor design." Science. 2016 Aug 5;353(6299):594-8. PMID:27493187
    6. Vandewynckel YP, Coucke C, et al. "Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma."Oncotarget. 2016 Jun 7;7(23):34988-5000. PMID:27167000

Oprozomib (ONX-0912)

Background

We Also Recommend

5-Aminovaleric acid hydrochloride

BIBR 1532

MEK162 (ARRY-162, ARRY-438162)