318262-42-9
Chemical Structure
NIK-12192
- CAS No.: 318262-42-9
- Formula:C26H31Cl2N3O2
- Molecular Weight:488.45
InChIKey: VNVUDBDBNZARAF-UHFFFAOYSA-N
SMILES: O=C(C1=CC(OCC)=C(C2=CC3=CC(Cl)=C(C=C3N2)Cl)C=C1)NC4CC(C)(C)NC(C)(C4)C
Biological Activity: NIK-12192 is an orally active inhibitor of vacuolar H+-ATPase. NIK-12192 reduces intracellular pH, decreases lysosomal volume and acidity, and alters the intracellular localization of V-ATPase by inhibiting proton pumps. NIK-12192 induces αvβ5 integrin polarization, cytoskeletal disruption, cell detachment, anoikis-mediated delayed apoptosis and necrosis, a delayed reduction in mitochondrial membrane potential, and lysosomal/phagosomal accumulation. NIK-12192 inhibits tumor cell migration, invasion, and three-dimensional spheroid growth, and enhances the activity of Topotecan (HY-13768). NIK-12192 suppresses spontaneous lung metastasis in vivo. NIK-12192 is used in research related to colon cancer, ovarian cancer, lung cancer, breast cancer, renal cancer, prostate cancer, acute myeloid leukemia, and melanoma[1][2].
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NIK-12192 | NIK-12192 is an orally active inhibitor of vacuolar H+-ATPase. NIK-12192 reduces intracellular pH, decreases lysosomal volume and acidity, and alters the intracellular localization of V-ATPase by inhibiting proton pumps. NIK-12192 induces αvβ5 integrin polarization, cytoskeletal disruption, cell detachment, anoikis-mediated delayed apoptosis and necrosis, a delayed reduction in mitochondrial membrane potential, and lysosomal/phagosomal accumulation. NIK-12192 inhibits tumor cell migration, invasion, and three-dimensional spheroid growth, and enhances the activity of Topotecan (HY-13768). NIK-12192 suppresses spontaneous lung metastasis in vivo. NIK-12192 is used in research related to colon cancer, ovarian cancer, lung cancer, breast cancer, renal cancer, prostate cancer, acute myeloid leukemia, and melanoma. | |||||||||||||||||||||
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References
- [1]. Supino R, et al. Biological effects of a new vacuolar-H,-ATPase inhibitor in colon carcinoma cell lines. Annals of the New York Academy of Sciences. 2009 Aug;1171:606-16.
- [2]. Supino R, et al. Antimetastatic effect of a small-molecule vacuolar H+-ATPase inhibitor in in vitro and in vivo preclinical studies. The Journal of pharmacology and experimental therapeutics. 2008 Jan;324(1):15-22.
