Description
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
Product information
CAS Number: 1202580-59-3
Molecular Weight: 439.55
Formula: C27H29N5O
Chemical Name: N-{[1,1'-biphenyl]-2-yl}-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide
Smiles: O=C(CCCCCCCN1C=C(N=N1)C1C=NC=CC=1)NC1C=CC=CC=1C1C=CC=CC=1
InChiKey: SJOLTIOPWDLDEB-UHFFFAOYSA-N
InChi: InChI=1S/C27H29N5O/c33-27(29-25-16-9-8-15-24(25)22-12-5-4-6-13-22)17-7-2-1-3-10-19-32-21-26(30-31-32)23-14-11-18-28-20-23/h4-6,8-9,11-16,18,20-21H,1-3,7,10,17,19H2,(H,29,33)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes. GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI50) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic.
In Vivo:
GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice.
Products are for research use only. Not for human use.
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