TCH-165 | 20S proteasome activator

CAS:
 1446350-60-2
Catalog Number:
 10-4400

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TCH-165 (1446350-60-2) is an activator of the 20S proteasome (EC50 = 4.2 µM).1 It enhanced the proteolysis of intrinsically disordered proteins, including α-synuclein, tau, ornithine decarboxylase, and c-Fos, without affecting structured proteins.  TCH-165 increased MYC degradation and reduced multiple myeloma and glioblastoma cell growth.2 It enhanced the degradation of neurotoxic dipeptide repeat proteins, protected rodent motor neurons, and restored proteostasis in cortical neuron cultures suggesting potential therapeutic use in neurodegenerative conditions.3 TCH-165 also attenuated cardiac ischemia/reperfusion injury in mice.4 Disruption of the MYC:MAX interaction by MYCMI-11 (Focus Cat#10-4146) along with 20S proteasome activation with TCH-165 enhanced MYC degradation, suppressed MYC-dependent transcription, and promoted apoptosis in colon cancer cells.5

References/Citations:

  1. Njomen et al. (2018) Small Molecule Modulation of Proteasome Assembly; Biochemistry 57 4214
  2. Njomen et al. (2022) Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma; Biomedicines 10 938
  3. Vanecek et al. (2023) Enhanced Degradation of Mutant C9ORF72-Derived Toxic Dipeptide Repeat Proteins by 20S Proteasome Activation Results in Restoration of Proteostasis and Neuroprotection; ACS Chem. Neurosci. 14 1439
  4. Gao et al. (2023) TCH-165 attenuates cardiac ischemia/reperfusion injury by balancing mitochondrial dynamics via increasing proteasome activity; Eur. J. Pharmacol. 957 176011
  5. Olatunde and Tepe (2026) Chemical Induction of MYC Protein Degradation via MYC-MAX Disruption and 20S Proteasome Activation; ACS Chem. Biol. 21 1728
1446350-60-2, 20S proteasome activator, MYC degradation, TCH-165, TCH-165 supplier, TCH165
CAS:
1446350-60-2
Catalog Number:
10-4400
Activity:
20S proteasome activator
Chemical Names:
Ethyl (4R,5R)-3-benzyl-4-[4-(benzylamino)phenyl]-2-(4-methoxyphenyl)-5-phenyl-4H-imidazole-5-carboxylate
Molecular Weight:
595.74
Molecular Formula:

C39H37N3O3

Solubility:
Soluble in DMSO (50 mg/ml)
Physical Properties:
Yellow solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

TCH-165 (1446350-60-2) is an activator of the 20S proteasome (EC50 = 4.2 µM).1 It enhanced the proteolysis of intrinsically disordered proteins, including α-synuclein, tau, ornithine decarboxylase, and c-Fos, without affecting structured proteins.  TCH-165 increased MYC degradation and reduced multiple myeloma and glioblastoma cell growth.2 It enhanced the degradation of neurotoxic dipeptide repeat proteins, protected rodent motor neurons, and restored proteostasis in cortical neuron cultures suggesting potential therapeutic use in neurodegenerative conditions.3 TCH-165 also attenuated cardiac ischemia/reperfusion injury in mice.4 Disruption of the MYC:MAX interaction by MYCMI-11 (Focus Cat#10-4146) along with 20S proteasome activation with TCH-165 enhanced MYC degradation, suppressed MYC-dependent transcription, and promoted apoptosis in colon cancer cells.5

References/Citations:

  1. Njomen et al. (2018) Small Molecule Modulation of Proteasome Assembly; Biochemistry 57 4214
  2. Njomen et al. (2022) Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma; Biomedicines 10 938
  3. Vanecek et al. (2023) Enhanced Degradation of Mutant C9ORF72-Derived Toxic Dipeptide Repeat Proteins by 20S Proteasome Activation Results in Restoration of Proteostasis and Neuroprotection; ACS Chem. Neurosci. 14 1439
  4. Gao et al. (2023) TCH-165 attenuates cardiac ischemia/reperfusion injury by balancing mitochondrial dynamics via increasing proteasome activity; Eur. J. Pharmacol. 957 176011
  5. Olatunde and Tepe (2026) Chemical Induction of MYC Protein Degradation via MYC-MAX Disruption and 20S Proteasome Activation; ACS Chem. Biol. 21 1728

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