2724212-01-3
Chemical Structure
KS-133
- CAS No.: 2724212-01-3
- Formula:C75H111N15O17S2
- Molecular Weight:1558.90
InChIKey: FCYHSMMFZBVBRY-FEBGRODTSA-N
SMILES: O=C(N(CCC1)[C@]1([H])C(N[C@H](C(N[C@H](C(N(CCC2)[C@]2([H])C3=O)=O)CC(C)C)=O)CC(C=C4)=CC=C4O)=O)[C@@](CCC5)([H])N5C([C@H](CSSC[C@@](NC([C@@H](NC([C@@H](NC6=O)CC(C=C7)=CC=C7O)=O)CC(C)C)=O)([H])C(N[C@@H](CC(NCCCC[C@]6([H])N3)=O)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)[C@@H](C)CC)=O)=O)=O)NC(C)=O)=O
Biological Activity: KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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KS-133 | 98.75% | KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer. | ||||||||||||||||||||
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References
- [1]. Sakamoto K, et al. Generation of KS-133 as a Novel Bicyclic Peptide with a Potent and Selective VIPR2 Antagonist Activity that Counteracts Cognitive Decline in a Mouse Model of Psychiatric Disorders. Front Pharmacol. 2021;12:751587. Published 2021 Nov 4. [Content Brief]
- [2]. Sakamoto K, et al. The VIPR2-selective antagonist KS-133 changes macrophage polarization and exerts potent anti-tumor effects as a single agent and in combination with an anti-PD-1 antibody. PLoS One. 2023;18(7):e0286651. Published 2023 Jul 5. [Content Brief]
- [3]. Sakamoto K, et al. Cyclic Peptides KS-133 and KS-487 Multifunctionalized Nanoparticles Enable Efficient Brain Targeting for Treating Schizophrenia. JACS Au. 2024;4(8):2811-2817. Published 2024 Jun 20. [Content Brief]
- [4]. Asano S, et al. Blockade of vasoactive intestinal peptide receptor 2 (VIPR2) signaling suppresses cyclin D1-dependent cell-cycle progression in MCF-7 cells. J Pharmacol Sci. 2024;154(3):139-147. [Content Brief]
