HLI98C | CAS# 317326-90-2 | MDM2 ubiquitin ligase inhibitor| MedKoo

MedKoo Cat#: 571063 | Name: HLI98C

Description:

WARNING: This product is for research use only, not for human or veterinary use.

HLI98C is a HDM2 ubiquitin ligase inhibitor. HLI98C exhibits cytotoxic activities and HDM2 E3 ligase inhibitory activities. In cells, HLI98C 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. HLI98C may demonstrate anti-tumor activity by inhibiting recognition of the E3 enzyme and substrate.

Chemical Structure

HLI98C

CAS#317326-90-2

Theoretical Analysis

MedKoo Cat#: 571063

Name: HLI98C

CAS#: 317326-90-2

Chemical Formula: C17H9ClN4O4

Exact Mass: 368.0312

Molecular Weight: 368.73

Elemental Analysis: C, 55.38; H, 2.46; Cl, 9.61; N, 15.19; O, 17.36

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

HLI98C; HLI-98C; HLI 98C.

IUPAC/Chemical Name

10-(3-chloro-phenyl)-7-nitro-10H-pyrimido[4,5-b]quinoline-2,4-dione

InChi Key

BRCGPVHRBGGGPW-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H9ClN4O4/c18-10-2-1-3-11(8-10)21-14-5-4-12(22(25)26)6-9(14)7-13-15(21)19-17(24)20-16(13)23/h1-8H,(H,20,23,24)

SMILES Code

O=C1N=C2N(C3=CC=CC(Cl)=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.

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 368.73 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

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.