HLI373


Catalog No. Size PriceQuantity
M12800-2 2mg solid $720
M12800-10 10mg solid $2,880

Description

HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.

Product information

CAS Number: 502137-98-6

Molecular Weight: 341.41

Formula: C18H23N5O2

Chemical Name: 5-{[3-(dimethylamino)propyl]amino}-3, 10-dimethyl-2H, 3H, 4H, 10H-pyrimido[4, 5-b]quinoline-2, 4-dione

Smiles: CN(C)CCCNC1=C2C(=NC(=O)N(C)C2=O)N(C)C2=CC=CC=C21

InChiKey: LNRUPMPQQGPSQT-UHFFFAOYSA-N

InChi: InChI=1S/C18H23N5O2/c1-21(2)11-7-10-19-15-12-8-5-6-9-13(12)22(3)16-14(15)17(24)23(4)18(25)20-16/h5-6,8-9,19H,7,10-11H2,1-4H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

HLI373 (3-15 μM; 15 hours) selectively kills tumor cells harboring wild type p53[1]. HLI373 (10-50 μM) stabilizes cellular Hdm2 in a dose-dependent manner. HLI373 (3 μM) activates p53 transcription. HLI373 selectively inhibits auto-ubiquitylation of Hdm2. Co-transfection with plasmids encoding p53 and Hdm2 results in degradation of p53. Incubation with HLI373 (5-10 μM; 8 hours) blocks p53 degradation. HLI373 increases p53 and Hdm2 protein levels in cells. HLI 373 also shows lower IC50 values (below 6 μM) against both chloroquine-sensitive P. falciparum D6 strain (PfD6) and chloroquine-resistant P. falciparum W2 strain (PfW2) and exhibits early growth inhibition. HLI-373 is a MDM2 inhibitor interrupting its ubiquitin E3 ligase activity, could abolish the ubiquitylation of its substrate protein p53. HLI-373 targets the C-terminus functioning as an E3 ubiquitin ligase.

References:

  1. Jirouta Kitagaki, et al. Targeting Tumor Cells Expressing p53 With a Water-Soluble Inhibitor of Hdm2. Mol Cancer Ther. 2008 Aug;7(8):2445-54.
  2. Jagrati Jain, et al. Inhibitors of Ubiquitin E3 Ligase as Potential New Antimalarial Drug Leads. BMC Pharmacol Toxicol. 2017 Jun 2;18(1):40.
  3. Ying Chen, et al. MDM2 Promotes Epithelial-Mesenchymal Transition and Metastasis of Ovarian Cancer SKOV3 Cells. Br J Cancer. 2017 Oct 10;117(8):1192-1201.

Products are for research use only. Not for human use.

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