2. Apoptosis Anti-infection
  3. MDM-2/p53 Parasite Apoptosis
  4. HLI373 dihydrochloride

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

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HLI373 dihydrochloride Chemical Structure

HLI373 dihydrochloride Chemical Structure

CAS No. : 1782531-99-0

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HLI373 dihydrochloride Related Antibodies

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Description

HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents[1]. Antimalarial activity[2].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HLI373 dihydrochloride Related Antibodies

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.
Molecular Weight

414.33

Formula

C18H25Cl2N5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N=C2N(C)C3=C(C=CC=C3)C(NCCCN(C)C)=C2C(N1C)=O.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 38 mg/mL (91.71 mM; Need ultrasonic and warming)

DMSO : 4 mg/mL (9.65 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4135 mL 12.0677 mL 24.1354 mL
5 mM 0.4827 mL 2.4135 mL 4.8271 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

COA (255 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.4135 mL 12.0677 mL 24.1354 mL 60.3384 mL
5 mM 0.4827 mL 2.4135 mL 4.8271 mL 12.0677 mL
H2O 10 mM 0.2414 mL 1.2068 mL 2.4135 mL 6.0338 mL
15 mM 0.1609 mL 0.8045 mL 1.6090 mL 4.0226 mL
20 mM 0.1207 mL 0.6034 mL 1.2068 mL 3.0169 mL
25 mM 0.0965 mL 0.4827 mL 0.9654 mL 2.4135 mL
30 mM 0.0805 mL 0.4023 mL 0.8045 mL 2.0113 mL
40 mM 0.0603 mL 0.3017 mL 0.6034 mL 1.5085 mL
50 mM 0.0483 mL 0.2414 mL 0.4827 mL 1.2068 mL
60 mM 0.0402 mL 0.2011 mL 0.4023 mL 1.0056 mL
80 mM 0.0302 mL 0.1508 mL 0.3017 mL 0.7542 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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HLI373 dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HLI3731782531-99-0HLI 373HLI-373MDM-2/p53ParasiteApoptosisHdm2ubiquitinligaseactivityapoptosistumorcellsAntimalarialp53embryofibroblastInhibitorinhibitorinhibit

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