Date published: 2025-11-3

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HLI 373 (CAS 502137-98-6)

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Alternate Names:
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione dihydrochloride; Hdm2 E3 Ligase Inhibitor II
Application:
HLI 373 is an apoptosis inducer and inhibitor of Hdm2 ubiquitin ligase
CAS Number:
502137-98-6
Purity:
≥98%
Molecular Weight:
414.32
Molecular Formula:
C18H23N5O22HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.

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HLI 373 is an inhibitor of Hdm2 ubiquitin ligase (E3) which blocks Hdm2-mediated ubiquitylation, proteasomal degradation of p53 and activates p53-dependent transcription. Additionally induces apoptosis in several tumor cell lines (LOX-IMVI, A549 and HT1080) expressing wild-type p53. HLI 373 is a substance that hinders the activity of Hdm2 ubiquitin ligase (E3), which is responsible for promoting the breakdown of p53 through a process called ubiquitylation, followed by degradation in the proteasome. By inhibiting Hdm2, HLI 373 prevents the ubiquitylation and subsequent degradation of p53, leading to the activation of p53-dependent transcription. As a result, HLI 373 induces apoptosis (cell death) specifically in various tumor cell lines that possess the wild-type p53 gene.


HLI 373 (CAS 502137-98-6) References

  1. Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2.  |  Kitagaki, J., et al. 2008. Mol Cancer Ther. 7: 2445-54. PMID: 18723490
  2. Targeting the ubiquitin-proteasome system for cancer therapy.  |  Yang, Y., et al. 2009. Cancer Sci. 100: 24-8. PMID: 19037995
  3. A comparative analysis of the ubiquitination kinetics of multiple degrons to identify an ideal targeting sequence for a proteasome reporter.  |  Melvin, AT., et al. 2013. PLoS One. 8: e78082. PMID: 24205101
  4. Inhibitors of ubiquitin E3 ligase as potential new antimalarial drug leads.  |  Jain, J., et al. 2017. BMC Pharmacol Toxicol. 18: 40. PMID: 28577368
  5. MDM2 promotes epithelial-mesenchymal transition and metastasis of ovarian cancer SKOV3 cells.  |  Chen, Y., et al. 2017. Br J Cancer. 117: 1192-1201. PMID: 28817834
  6. Ubiquitin-dependent proteolysis of CXCL7 leads to posterior longitudinal ligament ossification.  |  Tsuru, M., et al. 2018. PLoS One. 13: e0196204. PMID: 29782494
  7. Genetic alterations in anaplastic thyroid carcinoma and targeted therapies.  |  Li, Z., et al. 2019. Exp Ther Med. 18: 2369-2377. PMID: 31555347
  8. Carborane as an Alternative Efficient Hydrophobic Tag for Protein Degradation.  |  Asawa, Y., et al. 2021. Bioconjug Chem. 32: 2377-2385. PMID: 34699716
  9. Pharmacological Modulation of Ubiquitin-Proteasome Pathways in Oncogenic Signaling.  |  Sharma, A., et al. 2021. Int J Mol Sci. 22: PMID: 34769401
  10. MAGED2 Is Required under Hypoxia for cAMP Signaling by Inhibiting MDM2-Dependent Endocytosis of G-Alpha-S.  |  Seaayfan, E., et al. 2022. Cells. 11: PMID: 36010623
  11. Establishment and validation of a cholesterol metabolism-related prognostic signature for hepatocellular carcinoma.  |  Tang, L., et al. 2022. Comput Struct Biotechnol J. 20: 4402-4414. PMID: 36051877
  12. Development of single-molecule ubiquitination mediated fluorescence complementation to visualize protein ubiquitination dynamics in dendrites.  |  Ifrim, MF., et al. 2022. Cell Rep. 41: 111658. PMID: 36384114
  13. A Plasmodium falciparum RING Finger E3 Ubiquitin Ligase Modifies the Roles of PfMDR1 and PfCRT in Parasite Drug Responses.  |  Singh, BK., et al. 2023. Antimicrob Agents Chemother. 67: e0082122. PMID: 36625569

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

HLI 373, 10 mg

sc-358833
10 mg
$173.00
US: Only available in the US

HLI 373, 50 mg

sc-358833A
50 mg
$712.00
US: Only available in the US