2727965-45-7
Chemical Structure
Daporinad hydrochloride
Synonym(s): FK866 hydrochloride; APO866 hydrochloride
- CAS No.: 2727965-45-7
- Formula:C24H30ClN3O2
- Molecular Weight:427.97
InChIKey: MULSIBUGDPOSHV-CALJPSDSSA-N
SMILES: O=C(C1=CC=CC=C1)N2CCC(CC2)CCCCNC(/C=C/C3=CN=CC=C3)=O.Cl
Biological Activity: Daporinad (FK866) hydrochloride is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad hydrochloride depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad hydrochloride causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad hydrochloride induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad hydrochloride can be used for the study of myeloma, liver cancer, and immunosuppression[1][2][3][4].
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Daporinad hydrochloride | Daporinad (FK866) hydrochloride is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad hydrochloride depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad hydrochloride causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad hydrochloride induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad hydrochloride can be used for the study of myeloma, liver cancer, and immunosuppression. | |||||||||||||||||||||
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References
- [1]. Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29. [Content Brief]
- [2]. Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81. [Content Brief]
- [3]. Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7. [Content Brief]
- [4]. Hasmann M, Schemainda I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 2003 Nov 1;63(21):7436-42. [Content Brief]
