| Identification | Back Directory | [Name]
INGENOL-3-HEXANOATE | [CAS]
83036-61-7 | [Synonyms]
INGENOL-3-HEXANOATE
Hexanoic acid, (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2,5,5a,6,9,10,10a-octahydro-5,5a-dihydroxy-4-(hydroxymethyl)-1,1,7,9-tetramethyl-11-oxo-1H-2,8a-methanocyclopenta[a]cyclopropa[e]cyclodecen-6-yl ester | [Molecular Formula]
C26H38O6 | [MOL File]
83036-61-7.mol | [Molecular Weight]
446.58 |
| Hazard Information | Back Directory | [Description]
Ingenol 3-Hexanoate novel potent reactivator of latent HIV-1. | [Uses]
Ingenol 3-Hexanoate, an ingenol semi-synthetic derivative, is a potent anticancer agent. Ingenol 3-Hexanoate can be used in research of cancer[1]. | [in vitro]
One of the sgRNAs (LTR5), which binds specifically in the HIV-1 LTR NFκB binding site, was able to promote robust repression of HIV-1 reactivation in latently infected T cells stimulated with Phorbol 12-Myristate 13-Acetate (PMA) and Ingenol B (IngB), both potent protein kinase C (PKC) stimulators._x000D_
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Reference: Retrovirology. 2022 Jun 22;19(1):12. https://pubmed.ncbi.nlm.nih.gov/35733180/ | [in vivo]
However, significant toxicity risks and the lack of evidence supporting their activity in vivo have limited further evaluation of PKC agonists as HIV latency-reversing agents (LRA) in cure strategies. Here this study evaluated whether GSK445A, a stabilized ingenol-B derivative, can induce HIV/simian immunodeficiency virus (SIV) transcription and virus production in vitro and demonstrate pharmacological activity in nonhuman primates (NHP). In vivo, GSK445A tolerability was established in SIV-na?ve RM at 15 μg/kg although tolerability was reduced in SIV-infected RM on ART. Increases in plasma viremia following GSK445A administration were suggestive of increased SIV transcription in vivo. Collectively, these results indicate that GSK445A is a potent HIV/SIV LRA in vitro and has a tolerable safety profile amenable for further evaluation in vivo in NHP models of HIV cure/remission._x000D_
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Reference: PLoS Pathog. 2022 Jan 18;18(1):e1010245. https://pubmed.ncbi.nlm.nih.gov/35041707/ | [target]
Ingenol 3-Hexanoate, or Ingenol B, is a novel potent reactivator of latent HIV-1. | [References]
[1] Silva VAO, et, al. Modified ingenol semi-synthetic derivatives from Euphorbia tirucalli induce cytotoxicity on a large panel of human cancer cell lines. Invest New Drugs. 2019 Oct;37(5):1029-1035. DOI:10.1007/s10637-019-00728-0 |
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