Shanghai Nianxing Industrial Co., Ltd
China
Product Name: HLI 373
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

DC Chemicals Limited
China
Product Name: HLI373
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

ShangHai DC Chemicals Co.,Ltd
China
Product Name: HLI373
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

502137-98-6

502137-98-6 structure

Name: HLI 373
Chemical Name: 5-{[3-(Dimethylamino)propyl]amino}-3,10-dimethylpyrimido[4,5-b]qu inoline-2,4(3H,10H)-dione dihydrochloride
CAS Number: 502137-98-6
Molecular Formula: C₁₈H₂₃N₅O₂
Molecular Weight: 414.32900
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2016-10-08 01:57:12
Modify Date: 2024-03-07 17:52:08
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[1]. Antimalarial activity[2].

Name	5-{[3-(Dimethylamino)propyl]amino}-3,10-dimethylpyrimido[4,5-b]qu inoline-2,4(3H,10H)-dione dihydrochloride
Synonyms	MFCD30543744

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[1]. Antimalarial activity[2].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Research Areas >> Infection Signaling Pathways >> Apoptosis >> MDM-2/p53
Target	Hdm2[1]; Apoptosis[1]; Antimalarial[2]
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[1]. HLI373 selectively inhibits auto-ubiquitylation of Hdm2[1]. 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[1]. 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[2]. 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[3]. Cell Viability Assay[1] Cell Line: Wild type p53 mouse embryo fibroblasts (MEFs), and p53-deficient MEFs Concentration: 3, 10, 15 μM Incubation Time: 15 hours Result: Increased cell death in wild type p53 MEFs in a dose-dependent manner, p53-deficient MEFs were relatively resistant. Western Blot Analysis[1] Cell Line: U2OS cells Concentration: 5, 10 μM Incubation Time: 8 hours Result: Blocked p53 degradation caused by co-transfection with plasmids encoding p53 and Hdm2.
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.

Molecular Formula	C₁₈H₂₃N₅O₂
Molecular Weight	414.32900
Exact Mass	413.13900
PSA	72.16000
LogP	2.82600

Hazard Codes	Xi

1782531-99-0	502137-98-6
317326-90-2	14808-05-0
75696-02-5	84195-67-5
60630-67-3	574-66-3
13755-38-9	8009-03-8
1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4
2248390-52-3	2172319-31-0