STA-21 | CAS#111540-00-2 | STAT3 inhibitor

STA-21
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406525

CAS#: 111540-00-2

Description: STA-21 is a promising STAT-3 inhibitor that reciprocally regulates Th17 and Treg cells, inhibits osteoclastogenesis in mice and humans and alleviates autoimmune inflammation in an experimental model of rheumatoid arthritis. STA-21 improved the clinical course of arthritis in IL-1Ra-KO mice. It increased not only the number of Treg cells but also the function of the Treg cells. It also suppressed Th17 cells and osteoclast formation. These data suggest that STA-21 might be an effective treatment for patients with RA.

Chemical Structure

STA-21

CAS# 111540-00-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406525
Name: STA-21
CAS#: 111540-00-2
Chemical Formula: C19H14O4
Exact Mass: 306.09
Molecular Weight: 306.310
Elemental Analysis: C, 74.50; H, 4.61; O, 20.89

Price and Availability

Size	Price	Availability
1mg	USD 320	2 Weeks
5mg	USD 550	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: STA21; STA 21; STA21; Ochromycinone; NSC 628869.

IUPAC/Chemical Name: 8-hydroxy-3-methyl-3,4-dihydrotetraphene-1,7,12(2H)-trione

InChi Key: ZAWXOCUFQSQDJS-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H14O4/c1-9-7-10-5-6-12-17(15(10)14(21)8-9)19(23)11-3-2-4-13(20)16(11)18(12)22/h2-6,9,20H,7-8H2,1H3

SMILES Code: O=C1CC(C)CC2=CC=C3C(C(C4=CC=CC(O)=C4C3=O)=O)=C12

Appearance: white 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, not in water

Shelf Life: >2 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

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Product Data:

Product Data

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Biological target:	STA-21 is a natural antibiotic and a STAT3 inhibitor. STA-21 can inhibit STAT3 DNA binding activity and STAT3 dimerization.
In vitro activity:	STA-21 has potential in the treatment of rheumatoid arthritis (RA). STA-21 reduced the proportion of Th-17 cells and the expression of STAT3 target genes, RORγt, IL-21, and IL-23R involved in Th-17 cells differentiation while. Conversely, STA-21 conversely increased the proportion of Treg cells. STA-21 could reduce the expression of STAT3 target genes related to cell proliferation, apoptosis, and inflammation leading to a decrease in proliferation and conversely increase in apoptosis of RA-synovial fibroblasts. Reference: Int J Rheum Dis. 2024 Jan;27(1):e15032. https://pubmed.ncbi.nlm.nih.gov/38287543/
In vivo activity:	STA-21 has potential as a treatment strategy for the treatment of experimental autoimmune encephalomyelitis (EAE). In a mouse model, STA-21 ameliorated the EAE severity and decreased the EAE inflammation and demyelination. It also decreased STAT3 phosphorylation, the proportion of Th17 cells and the protein level of IL-17. STA-21 significantly decreased the expression of Th17 related transcription factors, RORɣt and IL-23R while FOXP3 expression associated with Treg differentiation was increased. Reference: Int Immunopharmacol. 2023 Jun;119:110160. https://pubmed.ncbi.nlm.nih.gov/37080068/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	16.7	54.42

Preparing Stock Solutions

The following data is based on the product molecular weight 306.31 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.

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:	1. Mohammad TAM, Hamad BK, Maroof AMA, Mahmud SO. STA-21 regulates Th-17/Treg balance and synovial fibroblasts functions in rheumatoid arthritis. Int J Rheum Dis. 2024 Jan;27(1):e15032. doi: 10.1111/1756-185X.15032. PMID: 38287543. 2. Wang L, Zhao J, Ren JP, Wu XY, Morrison ZD, Elgazzar MA, Ning SB, Moorman JP, Yao ZQ. Expansion of myeloid-derived suppressor cells promotes differentiation of regulatory T cells in HIV-1+ individuals. AIDS. 2016 Jun 19;30(10):1521-1531. doi: 10.1097/QAD.0000000000001083. PMID: 26959508; PMCID: PMC4889474. 3. Gharibi T, Barpour N, Hosseini A, Mohammadzadeh A, Marofi F, Ebrahimi-Kalan A, Nejati-Koshki K, Abdollahpour-Alitappeh M, Safaei S, Baghbani E, Baradaran B. STA-21, a small molecule STAT3 inhibitor, ameliorates experimental autoimmune encephalomyelitis by altering Th-17/Treg balance. Int Immunopharmacol. 2023 Jun;119:110160. doi: 10.1016/j.intimp.2023.110160. Epub 2023 Apr 18. Erratum in: Int Immunopharmacol. 2023 May 11;:110303. PMID: 37080068. 4. Nadeem A, Al-Harbi NO, Ansari MA, Al-Harbi MM, El-Sherbeeny AM, Zoheir KMA, Attia SM, Hafez MM, Al-Shabanah OA, Ahmad SF. Psoriatic inflammation enhances allergic airway inflammation through IL-23/STAT3 signaling in a murine model. Biochem Pharmacol. 2017 Jan 15;124:69-82. doi: 10.1016/j.bcp.2016.10.012. Epub 2016 Oct 28. PMID: 27984001.
In vitro protocol:	1. Mohammad TAM, Hamad BK, Maroof AMA, Mahmud SO. STA-21 regulates Th-17/Treg balance and synovial fibroblasts functions in rheumatoid arthritis. Int J Rheum Dis. 2024 Jan;27(1):e15032. doi: 10.1111/1756-185X.15032. PMID: 38287543. 2. Wang L, Zhao J, Ren JP, Wu XY, Morrison ZD, Elgazzar MA, Ning SB, Moorman JP, Yao ZQ. Expansion of myeloid-derived suppressor cells promotes differentiation of regulatory T cells in HIV-1+ individuals. AIDS. 2016 Jun 19;30(10):1521-1531. doi: 10.1097/QAD.0000000000001083. PMID: 26959508; PMCID: PMC4889474.
In vivo protocol:	1. Gharibi T, Barpour N, Hosseini A, Mohammadzadeh A, Marofi F, Ebrahimi-Kalan A, Nejati-Koshki K, Abdollahpour-Alitappeh M, Safaei S, Baghbani E, Baradaran B. STA-21, a small molecule STAT3 inhibitor, ameliorates experimental autoimmune encephalomyelitis by altering Th-17/Treg balance. Int Immunopharmacol. 2023 Jun;119:110160. doi: 10.1016/j.intimp.2023.110160. Epub 2023 Apr 18. Erratum in: Int Immunopharmacol. 2023 May 11;:110303. PMID: 37080068. 2. Nadeem A, Al-Harbi NO, Ansari MA, Al-Harbi MM, El-Sherbeeny AM, Zoheir KMA, Attia SM, Hafez MM, Al-Shabanah OA, Ahmad SF. Psoriatic inflammation enhances allergic airway inflammation through IL-23/STAT3 signaling in a murine model. Biochem Pharmacol. 2017 Jan 15;124:69-82. doi: 10.1016/j.bcp.2016.10.012. Epub 2016 Oct 28. PMID: 27984001.

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1: Park JS, Kwok SK, Lim MA, Kim EK, Ryu JG, Kim SM, Oh HJ, Ju JH, Park SH, Kim HY, Cho ML. STA-21, a promising STAT-3 inhibitor that reciprocally regulates Th17 and Treg cells, inhibits osteoclastogenesis in mice and humans and alleviates autoimmune inflammation in an experimental model of rheumatoid arthritis. Arthritis Rheumatol. 2014 Apr;66(4):918-29. doi: 10.1002/art.38305. PubMed PMID: 24757144.

2: Park JS, Kwok SK, Lim MA, Kim EK, Ryu JG, Kim SM, Oh HJ, Ju JH, Park SH, Kim HY, Cho ML. STA-21, a promising STAT3 inhibitor that reciprocally regulates Th17 and Treg, inhibits osteoclastogenesis and alleviates autoimmune inflammation. Arthritis Rheum. 2013 Dec 10. doi: 10.1002/art.38305. [Epub ahead of print] PubMed PMID: 24338788.

3: Miyoshi K, Takaishi M, Nakajima K, Ikeda M, Kanda T, Tarutani M, Iiyama T, Asao N, DiGiovanni J, Sano S. Stat3 as a therapeutic target for the treatment of psoriasis: a clinical feasibility study with STA-21, a Stat3 inhibitor. J Invest Dermatol. 2011 Jan;131(1):108-17. doi: 10.1038/jid.2010.255. Epub 2010 Sep 2. PubMed PMID: 20811392.

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