WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H571065
CAS#: NONE
Description: HLI98E is a HDM2 ubiquitin ligase inhibitor. HLI98E exhibits cytotoxic activities and HDM2 E3 ligase inhibitory activities. In cells, HLI98E allows the stabilization of p53 and HDM2 and activation of p53-dependent transcription and apoptosis. The p53 tumor suppressor protein is regulated by its interaction with HDM2, which serves as a ubiquitin ligase (E3) to target p53 for degradation. HLI98E may demonstrate anti-tumor activity by inhibiting recognition of the E3 enzyme and substrate.
Hodoodo Cat#: H571065
Name: HLI98E
CAS#: NONE
Chemical Formula: C18H12N4O4
Exact Mass: 348.09
Molecular Weight: 348.320
Elemental Analysis: C, 62.07; H, 3.47; N, 16.09; O, 18.37
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Related CAS #: 317326-90-2 (HLI98C)
Synonym: HLI98E; HLI 98E; HLI-98E
IUPAC/Chemical Name: 10-(4-methylphenyl)-7-nitro-10H-pyrimido[4,5-b]quinoline-2,4-dione
InChi Key: AHOQBMMKXUYLMD-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H12N4O4/c1-10-2-4-12(5-3-10)21-15-7-6-13(22(25)26)8-11(15)9-14-16(21)19-18(24)20-17(14)23/h2-9H,1H3,(H,20,23,24)
SMILES Code: O=C1N=C2N(C3=CC=C(C)C=C3)C4=C(C=C([N+]([O-])=O)C=C4)C=C2C(N1)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: The tumor suppressor protein p53 plays an important role in preventing cancer development by inhibiting the proliferation of cells undergoing tumorigenic stress, such as DNA damage or oncogene activation One of the principal E3s responsible for targeting the degradation of p53, and keeping p53 levels low during normal growth and development, is HDM2. In response to oncogenic stress, the degradation of p53 by HDM2 is inhibited, leading to a rapid increase in p53 protein levels in the cell, which is then controlled by degradation of normal p53 levels. The binding of HLI98 to HDM2 does not inhibit the interaction of HDM2 with p53, but appears to block the ubiquitylation and degradation of p53. In the protein ubiquitination cascade, ubiquitin (Ub) conjugation to a lysine residue on the target protein is catalyzed three enzymes: ubiquitin-activating enzyme (E1), ubiquitin conjugating enzyme (E2), and ubiquitin ligase (E3). In recent years, a variety of small-molecule inhibitors for ubiquitination have been discovered.
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The following data is based on the product molecular weight 348.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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1: Dou X, Li X, Tao L, Hu C, Zhang L, He Q, Yang B, Hu Y. Synthesis and biological evaluation of novel pyrimido[4,5-b]quinoline-2,4- dione derivatives as MDM2 ubiquitin ligase inhibitors. Med Chem. 2013 Jun 1;9(4):581-7. PubMed PMID: 22920093.
2: Yang Y, Ludwig RL, Jensen JP, Pierre SA, Medaglia MV, Davydov IV, Safiran YJ, Oberoi P, Kenten JH, Phillips AC, Weissman AM, Vousden KH. Small molecule inhibitors of HDM2 ubiquitin ligase activity stabilize and activate p53 in cells. Cancer Cell. 2005 Jun;7(6):547-59. PubMed PMID: 15950904.
3: Huang L, Hu B, Ni J, Wu J, Jiang W, Chen C, Yang L, Zeng Y, Wan R, Hu G, Wang X. Transcriptional repression of SOCS3 mediated by IL-6/STAT3 signaling via DNMT1 promotes pancreatic cancer growth and metastasis. J Exp Clin Cancer Res. 2016 Feb 4;35:27. doi: 10.1186/s13046-016-0301-7. PubMed PMID: 26847351; PubMed Central PMCID: PMC4743194.
4: Chen H, Wu G, Gao S, Guo R, Zhao Z, Yuan H, Liu S, Wu J, Lu X, Yuan X, Yu Z, Zu X, Xie N, Yang N, Hu Z, Sun Q, Zhang W. Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c from α-Santonin Derivatives. J Med Chem. 2017 Aug 2. doi: 10.1021/acs.jmedchem.6b01829. [Epub ahead of print] PubMed PMID: 28696694.
