1. Metabolic Enzyme/Protease
    Autophagy
  2. Nampt
    Autophagy
  3. GPP78

GPP78 (Synonyms: CAY10618)

Cat. No.: HY-14374
Handling Instructions

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.

For research use only. We do not sell to patients.

GPP78 Chemical Structure

GPP78 Chemical Structure

CAS No. : 1202580-59-3

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10 mM * 1 mL in DMSO USD 522 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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[1][2].

IC50 & Target

Nampt[1];
Autophagy[1]

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[1].
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[1].

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 10 nM
Incubation Time: 24 hours, 40 hours
Result: Punctate staining of LC3-II and the formation of autophagolysosomes were observable.
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[2].

Animal Model: Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result: Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.
Molecular Weight

439.55

Formula

C₂₇H₂₉N₅O

CAS No.

1202580-59-3

SMILES

O=C(CCCCCCCN1N=NC(C2=CN=CC=C2)=C1)NC3=CC=CC=C3C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GPP78CAY10618GPP 78GPP-78CAY 10618CAY-10618NamptAutophagyNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorCytotoxicityautophagyLC3-IIcellgrowthanti-canceranti-inflammatoryInhibitorinhibitorinhibit

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GPP78
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