ChemicalBook > CAS DataBase List > 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride

5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride

Product Name
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
CAS No.
502137-98-6
Chemical Name
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
Synonyms
HLI 373;Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione, 5-[[3-(dimethylamino)propyl]amino]-3,10-dimethyl-;5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
CBNumber
CB02518923
Molecular Formula
C18H23N5O2
Formula Weight
341.41
MOL File
502137-98-6.mol
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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride Property

storage temp. 
Desiccate at RT
solubility 
<37.79mg/ml in H2O;insoluble in DMSO
form 
solid
color 
Cream
Water Solubility 
water: 50mg/mL
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
373226
Product name
Hdm2 E3 Ligase Inhibitor II, HLI373 - CAS 502137-98-6 - Calbiochem
Packaging
5mg
Price
$154
Updated
2023/01/07
Tocris
Product number
3503
Product name
HLI373
Purity
≥99%(HPLC)
Packaging
10
Price
$174
Updated
2021/12/16
Tocris
Product number
3503
Product name
HLI373
Purity
≥99%(HPLC)
Packaging
50
Price
$721
Updated
2021/12/16
Usbiological
Product number
255456
Product name
HLI 373
Packaging
10mg
Price
$423
Updated
2021/12/16
ChemScene
Product number
CS-0029371
Product name
HLI373
Packaging
5mg
Price
$700
Updated
2021/12/16
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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride Chemical Properties,Usage,Production

Uses

HLI 373 is an apoptosis inducer and inhibitor of Hdm2 ubiquitin ligase.

Definition

ChEBI: 5-[3-(dimethylamino)propylamino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4-dione is an aminoquinoline.

Biological Activity

hli 373 is an inhibitor of hdm2 ubiquitin ligase (e3).hdm2 ubiquitin ligase(e3) is a major regulator of p53 by promoting its ubiquitylation and proteasomal degradation. therefore, blocking hdm2-mediated activities may be a therapeutic approach for cancers expressing wild-type p53 [1].

in vitro

hli373 effectively induces apoptosis of several tumor cells that are sensitive to dna-damaging agents. hli373-treated cells showed significantly more dna retained on the filter, indicating that it does not induce single-strand break in u2os cells. having no discernable effect on gp78 or ao7, hli373 seems prefer to inhibit the ubiquitin ligase activity of hdm2. treatment of u2os cells with hli373 at 10 amol/l also leaded to a marked decrease in ubiquitylated species immunoprecipitated with anti-hdm2, whereas the level of immunoprecipitated hdm2 increased. inhibition of hdm2-mediated ubiquitylation in cells can trigger stabilization of both p53 and hdm2 and preferential killing of tumor cells expressing wild-type p53. hli373 increased p53 through inhibiting hdm2-mediated ubiquitylation and not by inducing a dna damage response in u2os cells. hli373 has high potency in stabilizing hdm2 and p53. hli373 inhibits the ubiquitin ligase activity of hdm2 and induces a wild-type p53-dependent apoptosis in several tumor cells that are sensitive to dna-damaging agents [1,2].

References

[1]. kitagaki j, agama kk, pommier y, et al. targeting tumor cells expressing p53 with a water-soluble inhibitor of hdm2. molecular cancer therapeutics, 2008; 7(8): 2445-1454.
[2]. yang y, kitagaki j, wang h, hou dx, perantoni ao. targeting the ubiquitin-proteasome system for cancer therapy. cancer science, 2009, 100(1): 24-28.

5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride Suppliers

3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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86-21-50328109
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3bsc@sina.com
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China
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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EMMX Biotechnology LLC
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888-539-0666
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MedBioPharmaceutical Technology Inc
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Energy Chemical
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TargetMol Chemicals Inc.
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Shanghai Aladdin Biochemical Technology Co.,Ltd.
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Merck KGaA
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Adooq Bioscience LLC
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400-025-6535
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sales@adooq.cn
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Santa Cruz Biotechnology Inc
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021-60936350
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502137-98-6, 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochlorideRelated Search:


  • 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
  • HLI 373
  • Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione, 5-[[3-(dimethylamino)propyl]amino]-3,10-dimethyl-
  • 502137-98-6
  • C18H23N5O2HCl
  • C18H23N5O22HCl