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LTX-315

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

LTX-315, an oncolytic peptide with potent anticancer activity, kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization. LTX-315 inhibits MRC-5, A20 and AT84 with IC50s of 34.3, 8.3 and 11 µM, respectively.

Category

Peptide Inhibitors

Catalog number

BAT-010521

CAS number

1345407-05-7

Molecular Formula

C78H106N18O9

Molecular Weight

1439.79

Specification
Reference Reading

IUPAC Name

(2S)-2,6-diamino-N-[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxo-3,3-diphenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]hexanamide

Synonyms

LTX 315; LTX315; Ruxotemitide; H-Lys-Lys-Trp-Trp-Lys-Lys-Trp-Dip-Lys-NH2; L-lysyl-L-lysyl-L-tryptophyl-L-tryptophyl-L-lysyl-L-lysyl-L-tryptophyl-3,3-diphenyl-L-alanyl-L-lysinamide; Oncopore; (S)-2,6-diamino-N-((5S,8S,11S,14S,17S,20S,23S,26S)-11,20,23-tris((1H-indol-3-yl)methyl)-1,30-diamino-14,17-bis(4-aminobutyl)-8-benzhydryl-5-carbamoyl-7,10,13,16,19,22,25-heptaoxo-6,9,12,15,18,21,24-heptaazatriacontan-26-yl)hexanamide

Appearance

White Lyophilized Powder

Purity

≥95%

Density

1.263±0.06 g/cm3

Boiling Point

1700.2±65.0 °C at 760 Torr

Sequence

KKWWKKW-Dip-K-NH2

Storage

Store at -20°C

Solubility

Soluble in DMSO

InChI

1S/C78H106N18O9/c79-38-18-13-30-57(84)71(98)90-62(35-15-20-40-81)73(100)93-66(44-52-47-87-59-32-11-8-28-55(52)59)76(103)95-65(43-51-46-86-58-31-10-7-27-54(51)58)75(102)92-63(36-16-21-41-82)72(99)91-64(37-17-22-42-83)74(101)94-67(45-53-48-88-60-33-12-9-29-56(53)60)77(104)96-69(78(105)89-61(70(85)97)34-14-19-39-80)68(49-23-3-1-4-24-49)50-25-5-2-6-26-50/h1-12,23-29,31-33,46-48,57,61-69,86-88H,13-22,30,34-45,79-84H2,(H2,85,97)(H,89,105)(H,90,98)(H,91,99)(H,92,102)(H,93,100)(H,94,101)(H,95,103)(H,96,104)/t57-,61-,62-,63-,64-,65-,66-,67-,69-/m0/s1

InChI Key

GGAKLYWEFZCVIT-TVEKFXMRSA-N

Canonical SMILES

C1=CC=C(C=C1)C(C2=CC=CC=C2)C(C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCCCN)NC(=O)C(CCCCN)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CNC8=CC=CC=C87)NC(=O)C(CCCCN)NC(=O)C(CCCCN)N

1.Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315.

Camilio KA;Berge G;Ravuri CS;Rekdal O;Sveinbjørnsson B Cancer Immunol Immunother. 2014 Jun;63(6):601-13. doi: 10.1007/s00262-014-1540-0. Epub 2014 Mar 28.

Malignant melanoma is the most aggressive and deadliest form of skin cancer due to its highly metastatic potential, which calls for new and improved therapies. Cationic antimicrobial peptides (CAPs) are naturally occurring molecules found in most species, in which they play a significant role in the first line of defense against pathogens, and several CAPs have shown promising potential as novel anticancer agents. Structure-activity relationship studies on the CAP bovine lactoferricin allowed us to de novo design short chemically modified lytic anticancer peptides. In the present study, we investigated the in vivo antitumor effects of LTX-315 against intradermally established B16 melanomas in syngeneic mice. Intratumoral administration of LTX-315 resulted in tumor necrosis and the infiltration of immune cells into the tumor parenchyma followed by complete regression of the tumor in the majority of the animals. LTX-315 induced the release of danger-associated molecular pattern molecules such as the high mobility group box-1 protein in vitro and the subsequent upregulation of proinflammatory cytokines such as interleukin (IL) 1β, IL6 and IL18 in vivo. Animals cured by LTX-315 treatment were protected against a re-challenge with live B16 tumor cells both intradermally and intravenously.

2.The oncolytic peptide LTX-315 triggers immunogenic cell death.

Zhou H;Forveille S;Sauvat A;Yamazaki T;Senovilla L;Ma Y;Liu P;Yang H;Bezu L;Müller K;Zitvogel L;Rekdal Ø;Kepp O;Kroemer G Cell Death Dis. 2016 Mar 10;7:e2134. doi: 10.1038/cddis.2016.47.

LTX-315 is a cationic amphilytic peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis. Based on the observation that intratumorally injected LTX-315 stimulates a strong T lymphocyte-mediated anticancer immune response, we investigated whether LTX-315 may elicit the hallmarks of immunogenic cell death (ICD), namely (i) exposure of calreticulin on the plasma membrane surface, (ii) release of ATP into the extracellular space, (iii) exodus of HMGB1 from the nucleus, and (iv) induction of a type-1 interferon response. Using a panel of biosensor cell lines and robotized fluorescence microscopy coupled to automatic image analysis, we observed that LTX-315 induces all known ICD characteristics. This conclusion was validated by several independent methods including immunofluorescence stainings (for calreticulin), bioluminescence assays (for ATP), immunoassays (for HMGB1), and RT-PCRs (for type-1 interferon induction). When injected into established cancers, LTX-315 caused a transiently hemorrhagic focal necrosis that was accompanied by massive release of HMGB1 (from close-to-all cancer cells), as well as caspase-3 activation in a fraction of the cells.