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DHA (Dihydroartemisinin) NF-κB inhibitor

Name: DHA (Dihydroartemisinin)
Brand: Selleck Chemicals
SKU: S2290
Availability: InStock
Rating: 5 (35 reviews)

Cat.No.S2290

Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin, is isolated from the traditional Chinese herb Artemisia annua. It induces autophagy and apoptosis by suppressing NF-κB activation.

Chemical Structure

Molecular Weight: 284.35

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99%

Related Targets	Antioxidant HDAC ROS IκB/IKK Nrf2 AP-1 MALT NOD
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Chemical Information, Storage & Stability

Molecular Weight	284.35	Formula	C₁₅H₂₄O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	71939-50-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (49.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	6%DMSO 1 94%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (10.55mM)	Taking the 1 mL working solution as an example, add 60 μL of 50 mg/ml clear DMSO stock solution to 940 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%H2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (14.07mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB ^[4]
In vitro	Dihydroartemisinin (DHA) inhibits the growth of certain cancer cell lines and xenograft tumors such as leukemia, glioma, fibrosarcoma, and breast, cervical, ovarian, lung, oral and pancreatic cancer. It inhibits cell and tumor growth by modulating various tumor-suppressive pathways, such as inhibiting cell proliferation and inducing apoptosis through regulation of proliferation- and apoptosis-related proteins.This compound inhibits the proliferation and viability of cells in a dose-dependent manner and induces apoptosis.Its mediated cytotoxicity is tumor selective. The endoperoxide bridge of DHA is reportedly essential for its cytotoxicity because it reacts with intracellular ferrous iron to generate reactive oxygen species or carbon-centered radicals, leading to cytotoxicity^[1].
In vivo	DHA (Dihydroartemisinin) significantly inhibited HCC cell growth in vitro and in vivo via inducing G2/M cell cycle arrest and apoptosis^[2]. In the rat whole embryo culture (WEC), this compound has been shown to primarily affect primitive red blood cells (RBCs) causing subsequent tissue damage and dysmorphogenesis^[3].
References	[1] https://pubmed.ncbi.nlm.nih.gov/21617209/ [2] https://pubmed.ncbi.nlm.nih.gov/22342732/ [3] https://pubmed.ncbi.nlm.nih.gov/16959470/ [4] https://pubmed.ncbi.nlm.nih.gov/24099910/

Applications

Methods	Biomarkers	PMID
Western blot	p-STAT3 / p-JAK2 MMP-2 / MMP-9 E-cadherin / N-cadherin / Vimentin / Twist / Slug / Snail	29434895
Immunofluorescence	PDGFRα	29387451
Growth inhibition assay	Cell viability	29114376

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06274788	Not yet recruiting	Parenteral Nutrition Associated Liver Disease (PNALD)\|Essential Fatty Acid Deficiency\|Malnutrition\|Pediatric ALL	Fresenius Kabi	May 1 2024	Phase 4
NCT06319079	Not yet recruiting	Lactating Mothers\|Infants	Instituto de Desarrollo e Investigaciones Pediátricas Prof. Dr. Fernando E. Viteri	March 2024	Not Applicable

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