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HOME> Products> Natural and Chemical compound> Fluostatin A, B
HOME> Products> Natural and Chemical compound> Enzyme inhibitor> Fluostatin A, B

Dipeptidyl Peptidase III (DPP-III) Inhibitor Fluostatin A, B

Date：April 14 2022Web Page No：95022

Institute of Microbial Chemistry

Fluostatin A (Sodium Salt) and Fluostatin B is a natural compound derived from actinomycetes, and thye are selective inhibitors for human placental dipeptidyl peptidase III (DPP-III, DPP3)^{1, 2)}. Fluostatin A is reported to be about 50 times more active against human DPP III than its homologue Fluostatin B.

What is DPP III
Specification
Inhibitory activity against DPP enzyme subtype
References

What is DPP III

Dipeptidyl peptidase III (DPP III), a zinc-dependent aminopeptidase, is an enzyme involved in cleaving dipeptides from the N-terminus of tetra- to decapeptides, thereby taking part in activation as well as degradation of signalling peptides critical in physiological and pathological processes such as blood pressure regulation, nociception, inflammation and cancer.
DPP III is said to function as a regulator of the cellular oxidative stress response pathways, such as the Keap1-Nrf2-mediated antioxidative respons, and as a key modulator of the renin-angiotensin system related to blood pressure regulation. In addition, since DPP III degrades enkephalin, it is also known as enkephalinase B, so it has been suggested to be involved in the regulation of pain, and has attracted attention as a drug discovery target.

Reference

Malovan, G., et al., FEBS J., Mar. 12 (2022) doi: 10.1111/febs.16429. [PMID:35278345]

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Specification

Name	Fluostatin A (Sodium Salt)	Fluostatin B
Code	15403	14683
Structure
Overview	Fluostatin A was prepared from fluostatin B by chemical dehydration and oxidation. Inhibits human placental DPP-III selectively (IC₅₀: 0.44 μg/mL)¹⁾. No toxicity after intraperitoneal injection in mice at a dose of 100 mg/kg. ¹⁾	Fluostatin B is derived from Streptomyces sp. TA-3391. Inhibits human placental DPP-III selectively (IC₅₀: 24 ug/mL)¹⁾. No toxicity after intraperitoneal injection in mice at a dose of 100 mg/kg. ¹⁾
Purity	>98% (HPLC)	>98% (HPLC)
CAS No.	160219-74-9 (salt free form) ^*	158906-40-2
Molecular Formula	C₁₈H₉O₅ Na (sodium salt)	C₁₈H₁₄O₆
Molecular Weight	328.225	326.304
Solubility	Soluble in H2O, DMSO Poorly soluble in MeOH	Soluble in DMSO, partially soluble in EtOAc, Acetone Insoluble in H2O

* Fluostatin A is supplied as sodium salt.

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Inhibitory activity against DPP enzyme subtype

Name		Fluostatin A (Sodium Salt)	Fluostatin B
Code		15403	14683
IC₅₀ （μg/ml）	DPPⅠ	＞100	＞100
	DPPⅡ	＞100	＞100
	DPPⅢ	0.44	24.00
	DPPⅣ	＞100	＞100

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References

Akiyama, T., et al., J. Antibiot., 51 (6), 553～559 (1998). [PMID:9711218]
Akiyama, T., et al., J. Antibiot., 51 (6), 586～588 (1998). [PMID:9711223]

[Date : January 13 2025 00:06]

Detail Product Name Product Code Supplier Size Price

Fluostatin A (sodium salt), Dipeptidyl Peptidase Ⅲ (DPP-Ⅲ) Inhibitor
DatasheetThis may not be the latest data sheet. 15403 IMCInstitute of Microbial Chemistry 1 mg $500

Contact

Description
Storage	-20°C	CAS	160219-74-9 (salt free form)
Link	Bioactive Compounds

Fluostatin B, Dipeptidyl Peptidase III (DPP-III) Inhibitor
DatasheetThis may not be the latest data sheet. 14683 IMCInstitute of Microbial Chemistry 1 mg $500

Contact

Description
Storage	-20°C	CAS	158906-40-2
Link	Bioactive Compounds

[Date : January 13 2025 00:06]

Fluostatin A (sodium salt), Dipeptidyl Peptidase Ⅲ (DPP-Ⅲ) Inhibitor

DatasheetThis may not be the latest data sheet.

Product Code: 15403
Supplier: IMC
Size: 1mg
Price: $500

Description
Storage	-20°C	CAS	160219-74-9 (salt free form)
Link	Bioactive Compounds

Contact

Fluostatin B, Dipeptidyl Peptidase III (DPP-III) Inhibitor

DatasheetThis may not be the latest data sheet.

Product Code: 14683
Supplier: IMC
Size: 1mg
Price: $500

Description
Storage	-20°C	CAS	158906-40-2
Link	Bioactive Compounds

Contact

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