AKB-4924

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555804

CAS#: Unknown

Description: AKB-4924, also known as,GB004, is a selective stabilizer HIF-1 alpha for the treatment of inflammatory bowel disease. HIF-1 alpha is involved in mucosal wound healing and the reduction of inflammation in the gastrointestinal tract. AKB-4924 increases HIF-1 levels and enhances the antibacterial activity of phagocytes and keratinocytes against both methicillin-sensitive and methicillin-resistant strains of Staphylococcus aureus in vitro. AKB-4924 is also effective in stimulating the killing capacity of keratinocytes against the important opportunistic skin pathogens Pseudomonas aeruginosa and Acinetobacter baumanii.

Chemical Structure

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AKB-4924
CAS# Unknown
Instruction

Theoretical Analysis

MedKoo Cat#: 555804
Name: AKB-4924
CAS#: Unknown
Chemical Formula:
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis:

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: AKB-4924; AKB 4924; AKB4924;

IUPAC/Chemical Name: N/A

InChi Key:

InChi Code:

SMILES Code:

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Uropathogenic E. coli (UPEC) is the primary cause of urinary tract infections (UTI) affecting approximately 150 million people worldwide. Here, we revealed the importance of transcriptional regulator hypoxia-inducible factor-1 α subunit (HIF-1α) in innate defense against UPEC-mediated UTI. Hypoxia inducible factor-1 (HIF-1) is a transcription factor that is a major regulator of energy homeostasis and cellular adaptation to low oxygen stress. HIF-1 is also activated in response to bacterial pathogens and supports the innate immune response of both phagocytes and keratinocytes

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 0.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Grover SP, Saha P, Humphries J, Lyons OT, Patel AS, Serneels J, Modarai B, Mazzone M, Smith A. Inhibition of prolyl hydroxylase domain proteins selectively enhances venous thrombus neovascularisation. Thromb Res. 2018 Sep;169:105-112. doi: 10.1016/j.thromres.2018.07.015. Epub 2018 Jul 11. PMID: 30031289.


2: Gupta N, Nizet V. Stabilization of Hypoxia-Inducible Factor-1 Alpha Augments the Therapeutic Capacity of Bone Marrow-Derived Mesenchymal Stem Cells in Experimental Pneumonia. Front Med (Lausanne). 2018 May 4;5:131. doi: 10.3389/fmed.2018.00131. PMID: 29780805; PMCID: PMC5945808.


3: Branitzki-Heinemann K, Möllerherm H, Völlger L, Husein DM, de Buhr N, Blodkamp S, Reuner F, Brogden G, Naim HY, von Köckritz-Blickwede M. Formation of Neutrophil Extracellular Traps under Low Oxygen Level. Front Immunol. 2016 Nov 25;7:518. doi: 10.3389/fimmu.2016.00518. PMID: 27933059; PMCID: PMC5122589.


4: Lin AE, Beasley FC, Olson J, Keller N, Shalwitz RA, Hannan TJ, Hultgren SJ, Nizet V. Role of Hypoxia Inducible Factor-1α (HIF-1α) in Innate Defense against Uropathogenic Escherichia coli Infection. PLoS Pathog. 2015 Apr 30;11(4):e1004818. doi: 10.1371/journal.ppat.1004818. PMID: 25927232; PMCID: PMC4415805.


5: Marks E, Goggins BJ, Cardona J, Cole S, Minahan K, Mateer S, Walker MM, Shalwitz R, Keely S. Oral delivery of prolyl hydroxylase inhibitor: AKB-4924 promotes localized mucosal healing in a mouse model of colitis. Inflamm Bowel Dis. 2015 Feb;21(2):267-75. doi: 10.1097/MIB.0000000000000277. PMID: 25545377.


6: Leire E, Olson J, Isaacs H, Nizet V, Hollands A. Role of hypoxia inducible factor-1 in keratinocyte inflammatory response and neutrophil recruitment. J Inflamm (Lond). 2013 Aug 10;10(1):28. doi: 10.1186/1476-9255-10-28. PMID: 23937964; PMCID: PMC3751314.


7: Keely S, Campbell EL, Baird AW, Hansbro PM, Shalwitz RA, Kotsakis A, McNamee EN, Eltzschig HK, Kominsky DJ, Colgan SP. Contribution of epithelial innate immunity to systemic protection afforded by prolyl hydroxylase inhibition in murine colitis. Mucosal Immunol. 2014 Jan;7(1):114-23. doi: 10.1038/mi.2013.29. Epub 2013 May 22. PMID: 23695513; PMCID: PMC3772994.


8: Bhandari T, Olson J, Johnson RS, Nizet V. HIF-1α influences myeloid cell antigen presentation and response to subcutaneous OVA vaccination. J Mol Med (Berl). 2013 Oct;91(10):1199-205. doi: 10.1007/s00109-013-1052-y. Epub 2013 May 19. PMID: 23686259; PMCID: PMC3783576.


9: Branitzki-Heinemann K, Okumura CY, Völlger L, Kawakami Y, Kawakami T, Naim HY, Nizet V, Von Köckritz-Blickwede M. A novel role for the transcription factor HIF-1α in the formation of mast cell extracellular traps. Biochem J. 2012 Aug 15;446(1):159-63. doi: 10.1042/BJ20120658. PMID: 22738198; PMCID: PMC3606900.


10: Okumura CY, Hollands A, Tran DN, Olson J, Dahesh S, von Köckritz-Blickwede M, Thienphrapa W, Corle C, Jeung SN, Kotsakis A, Shalwitz RA, Johnson RS, Nizet V. A new pharmacological agent (AKB-4924) stabilizes hypoxia inducible factor-1 (HIF-1) and increases skin innate defenses against bacterial infection. J Mol Med (Berl). 2012 Sep;90(9):1079-89. doi: 10.1007/s00109-012-0882-3. Epub 2012 Feb 28. PMID: 22371073; PMCID: PMC3606899.