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Cyclosporin H

ALX-380-286

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TPA/PMA inhibitor

Immunologically inactive. Does not bind to immunophilin. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. BML-PE160) in mouse skin in vivo. Potent inhibitor of Ca²⁺/calmodulin dependent EF-2 phosphorylation in vitro. Potent and selective antagonist of formyl peptide receptor. Inhibits formyl peptide-induced superoxide formation.

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Product Details

Alternative Name	Csh-cyclosporin, 5-(N-Methyl-D-valine)-cyclosporin A
Appearance	White to off-white powder.
CAS	83602-39-5
Couple Target	Formyl peptide receptor, PMA
Couple Type	Inhibitor
Formula	C₆₂H₁₁₁N₁₁O₁₂
MW	1202.6
Purity	≥95% (HPLC)
Solubility	Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
Source	Isolated from Tolypocladium inflatum.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

2-Deoxy-D-glucose couples mitochondrial DNA replication with mitochondrial fitness and promotes the selection of wild-type over mutant mitochondrial DNA: B. Pantic, et al.; Nat. Commun. 12, 6997 (2021), Abstract
G-protein-coupled formyl peptide receptors play a dual role in neutrophil chemotaxis and bacterial phagocytosis: Wen, X., Xu, X., et al.; Mol. Biol. Cell 30, 346 (2019), Abstract
The role of formyl peptide receptor 1 (FPR1) in neuroblastoma tumorigenesis: I. Snapkov, et al.; BMC Cancer 16, 490 (2016), Application(s): Inhibition of FPR1 signaling and Ca2+ mobilization, Abstract — Full Text
Antimicrobial peptide scolopendrasin VII, derived from the centipede Scolopendra subspinipes mutilans, stimulates macrophage chemotaxis via formyl peptide receptor 1: Y. J. Park, et al.; BMB Rep. 48, 479 (2015), Application(s): Cell Culture, Abstract — Full Text
Functional characteristics of the Staphylococcus aureus δ-toxin allelic variant G10S: G.Y. Cheung, et al.; Sci. Rep. 5, 18023 (2015), Application(s): Cell culture, Abstract — Full Text
Distinct signalling mechanisms mediate neutrophil attraction to bacterial infection and tissue injury: Deng, Q., Harvie, E. A., et al.; Cell. Microbiol. 14, 517 (2012), Abstract
Cyclosporin H, Boc-MLF and Boc-FLFLF are antagonists that preferentially inhibit activity triggered through the formyl peptide receptor: A.L. Stenfeldt, et al.; Inflammation 30, 224 (2007), Abstract
Cyclosporin H is a potent and selective competitive antagonist of human basophil activation by N-formyl-methionyl-leucyl-phenylalanine: A. de Paulis, et al.; J. Allergy Clin. Immunol. 98, 152 (1996), Abstract
Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E: K. Wenzel-Seifert & R. Seifert; J. Immunol. 150, 4591 (1993), Abstract
Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation: K. Wenzel-Seifert, et al.; J. Immunol. 147, 1940 (1991), Abstract

Related Products

Phorbol 12-myristate 13-acetate

BML-PE160

PKC activator

59 citations

Alternative Name	PMA, TPA
CAS	16561-29-8
Couple Type	Activator
Purity	≥99% (HPLC, TLC)

Last modified: May 29, 2024

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Cyclosporin H

ALX-380-286

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