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

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.

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GPP78 Chemical Structure

GPP78 Chemical Structure

CAS No. : 1202580-59-3

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5 mg (11.38 mM * 1 mL in Methanol) In-stock
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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]

Cellular Effect
Cell Line Type Value Description References
786-0 GI50
7.33 μM
Compound: 8
Growth inhibition of human 786-0 cells by sulforhodamine B assay
Growth inhibition of human 786-0 cells by sulforhodamine B assay
[PMID: 19961183]
A498 GI50
1.59 x 10-5 M
Compound: 8
Growth inhibition of human A498 cells by sulforhodamine B assay
Growth inhibition of human A498 cells by sulforhodamine B assay
[PMID: 19961183]
A549 GI50
2.1 μM
Compound: 8
Growth inhibition of human A549 cells by sulforhodamine B assay
Growth inhibition of human A549 cells by sulforhodamine B assay
[PMID: 19961183]
ACHN GI50
1.87 x 10-5 M
Compound: 8
Growth inhibition of human ACHN cells by sulforhodamine B assay
Growth inhibition of human ACHN cells by sulforhodamine B assay
[PMID: 19961183]
BT-549 GI50
1.7 μM
Compound: 8
Growth inhibition of human BT549 cells by sulforhodamine B assay
Growth inhibition of human BT549 cells by sulforhodamine B assay
[PMID: 19961183]
CAKI-1 GI50
7.76 x 10-1 μM
Compound: 8
Growth inhibition of human Caki1 cells by sulforhodamine B assay
Growth inhibition of human Caki1 cells by sulforhodamine B assay
[PMID: 19961183]
CCRF-CEM GI50
3.28 μM
Compound: 8
Growth inhibition of human CCRF-CEM cells by sulforhodamine B assay
Growth inhibition of human CCRF-CEM cells by sulforhodamine B assay
[PMID: 19961183]
COLO 205 GI50
1.18 μM
Compound: 8
Growth inhibition of human COLO205 cells by sulforhodamine B assay
Growth inhibition of human COLO205 cells by sulforhodamine B assay
[PMID: 19961183]
DU-145 GI50
7.02 x 10-1 μM
Compound: 8
Growth inhibition of human DU145 cells by sulforhodamine B assay
Growth inhibition of human DU145 cells by sulforhodamine B assay
[PMID: 19961183]
EKVX GI50
8.46 μM
Compound: 8
Growth inhibition of human EKVX cells by sulforhodamine B assay
Growth inhibition of human EKVX cells by sulforhodamine B assay
[PMID: 19961183]
HCC 2998 GI50
7 x 10-1 μM
Compound: 8
Growth inhibition of human HCC2998 cells by sulforhodamine B assay
Growth inhibition of human HCC2998 cells by sulforhodamine B assay
[PMID: 19961183]
HCT-116 GI50
4.03 x 10-2 μM
Compound: 8
Growth inhibition of human HCT116 cells by sulforhodamine B assay
Growth inhibition of human HCT116 cells by sulforhodamine B assay
[PMID: 19961183]
HCT-15 GI50
2.57 x 10-1 μM
Compound: 8
Growth inhibition of human HCT15 cells by sulforhodamine B assay
Growth inhibition of human HCT15 cells by sulforhodamine B assay
[PMID: 19961183]
HOP-62 GI50
2.38 x 10-5 M
Compound: 8
Growth inhibition of human HOP62 cells by sulforhodamine B assay
Growth inhibition of human HOP62 cells by sulforhodamine B assay
[PMID: 19961183]
HOP-92 GI50
9.74 x 10-5 M
Compound: 8
Growth inhibition of human HOP92 cells by sulforhodamine B assay
Growth inhibition of human HOP92 cells by sulforhodamine B assay
[PMID: 19961183]
Hs-578T GI50
2.04 x 10-5 M
Compound: 8
Growth inhibition of human Hs 578T cells by sulforhodamine B assay
Growth inhibition of human Hs 578T cells by sulforhodamine B assay
[PMID: 19961183]
HT-29 GI50
4.6 x 10-1 μM
Compound: 8
Growth inhibition of human HT-29 cells by sulforhodamine B assay
Growth inhibition of human HT-29 cells by sulforhodamine B assay
[PMID: 19961183]
IGROV-1 GI50
2.72 x 10-1 μM
Compound: 8
Growth inhibition of human IGROV1 cells by sulforhodamine B assay
Growth inhibition of human IGROV1 cells by sulforhodamine B assay
[PMID: 19961183]
KM12 GI50
1.03 μM
Compound: 8
Growth inhibition of human KM12 cells by sulforhodamine B assay
Growth inhibition of human KM12 cells by sulforhodamine B assay
[PMID: 19961183]
LOX IMVI GI50
1.01 x 10-5 M
Compound: 8
Growth inhibition of human LOXIMVI cells by sulforhodamine B assay
Growth inhibition of human LOXIMVI cells by sulforhodamine B assay
[PMID: 19961183]
M14 GI50
1.66 x 10-1 μM
Compound: 8
Growth inhibition of human M14 cells by sulforhodamine B assay
Growth inhibition of human M14 cells by sulforhodamine B assay
[PMID: 19961183]
Malme-3M GI50
1.22 x 10-5 M
Compound: 8
Growth inhibition of human MALME-3M cells by sulforhodamine B assay
Growth inhibition of human MALME-3M cells by sulforhodamine B assay
[PMID: 19961183]
MCF7 GI50
3.42 μM
Compound: 8
Growth inhibition of human MCF7 cells by sulforhodamine B assay
Growth inhibition of human MCF7 cells by sulforhodamine B assay
[PMID: 19961183]
MDA-MB-231 GI50
2.09 x 10-5 M
Compound: 8
Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay
Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay
[PMID: 19961183]
MDA-MB-435 GI50
3.99 x 10-1 μM
Compound: 8
Growth inhibition of human MDA-MB-435 cells by sulforhodamine B assay
Growth inhibition of human MDA-MB-435 cells by sulforhodamine B assay
[PMID: 19961183]
MDA-MB-468 GI50
7.34 μM
Compound: 8
Growth inhibition of human MDA-MB-468 cells by sulforhodamine B assay
Growth inhibition of human MDA-MB-468 cells by sulforhodamine B assay
[PMID: 19961183]
NCI/ADR-RES GI50
8.14 x 10-2 μM
Compound: 8
Growth inhibition of human NCI/ADR-RES cells by sulforhodamine B assay
Growth inhibition of human NCI/ADR-RES cells by sulforhodamine B assay
[PMID: 19961183]
NCI-H226 GI50
1.55 x 10-5 M
Compound: 8
Growth inhibition of human NCI-H226 cells by sulforhodamine B assay
Growth inhibition of human NCI-H226 cells by sulforhodamine B assay
[PMID: 19961183]
NCI-H23 GI50
1.51 x 10-5 M
Compound: 8
Growth inhibition of human NCI-H23 cells by sulforhodamine B assay
Growth inhibition of human NCI-H23 cells by sulforhodamine B assay
[PMID: 19961183]
NCI-H322M GI50
2.31 x 10-5 M
Compound: 8
Growth inhibition of human NCI-H322M cells by sulforhodamine B assay
Growth inhibition of human NCI-H322M cells by sulforhodamine B assay
[PMID: 19961183]
NCI-H460 GI50
7.24 x 10-1 μM
Compound: 8
Growth inhibition of human NCI-H460 cells by sulforhodamine B assay
Growth inhibition of human NCI-H460 cells by sulforhodamine B assay
[PMID: 19961183]
NCI-H522 GI50
9.14 x 10-2 μM
Compound: 8
Growth inhibition of human NCI-H522 cells by sulforhodamine B assay
Growth inhibition of human NCI-H522 cells by sulforhodamine B assay
[PMID: 19961183]
OVCAR-3 GI50
5.19 μM
Compound: 8
Growth inhibition of human OVCAR-3 cells by sulforhodamine B assay
Growth inhibition of human OVCAR-3 cells by sulforhodamine B assay
[PMID: 19961183]
OVCAR-4 GI50
3.16 x 10-5 M
Compound: 8
Growth inhibition of human OVCAR4 cells by sulforhodamine B assay
Growth inhibition of human OVCAR4 cells by sulforhodamine B assay
[PMID: 19961183]
OVCAR-5 GI50
2.68 x 10-1 μM
Compound: 8
Growth inhibition of human OVCAR5 cells by sulforhodamine B assay
Growth inhibition of human OVCAR5 cells by sulforhodamine B assay
[PMID: 19961183]
OVCAR-8 GI50
5.74 x 10-2 μM
Compound: 8
Growth inhibition of human OVCAR8 cells by sulforhodamine B assay
Growth inhibition of human OVCAR8 cells by sulforhodamine B assay
[PMID: 19961183]
PC-3 GI50
4.67 x 10-1 μM
Compound: 8
Growth inhibition of human PC3 cells by sulforhodamine B assay
Growth inhibition of human PC3 cells by sulforhodamine B assay
[PMID: 19961183]
RXF 393 GI50
1 x 10-4 M
Compound: 8
Growth inhibition of human RXF393 cells by sulforhodamine B assay
Growth inhibition of human RXF393 cells by sulforhodamine B assay
[PMID: 19961183]
SF-268 GI50
2.47 x 10-5 M
Compound: 8
Growth inhibition of human SF268 cells by sulforhodamine B assay
Growth inhibition of human SF268 cells by sulforhodamine B assay
[PMID: 19961183]
SF-295 GI50
6.55 x 10-1 μM
Compound: 8
Growth inhibition of human SF295 cells by sulforhodamine B assay
Growth inhibition of human SF295 cells by sulforhodamine B assay
[PMID: 19961183]
SF-539 GI50
6.18 x 10-2 μM
Compound: 8
Growth inhibition of human SF539 cells by sulforhodamine B assay
Growth inhibition of human SF539 cells by sulforhodamine B assay
[PMID: 19961183]
SH-SY5Y IC50
3.8 nM
Compound: 8
Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 19961183]
SK-MEL-2 GI50
1.28 x 10-5 M
Compound: 8
Growth inhibition of human SK-MEL-2 cells by sulforhodamine B assay
Growth inhibition of human SK-MEL-2 cells by sulforhodamine B assay
[PMID: 19961183]
SK-MEL-28 GI50
1.59 μM
Compound: 8
Growth inhibition of human SK-MEL-28 cells by sulforhodamine B assay
Growth inhibition of human SK-MEL-28 cells by sulforhodamine B assay
[PMID: 19961183]
SK-MEL-5 GI50
2.64 x 10-5 M
Compound: 8
Growth inhibition of human SK-MEL-5 cells by sulforhodamine B assay
Growth inhibition of human SK-MEL-5 cells by sulforhodamine B assay
[PMID: 19961183]
SK-OV-3 GI50
2.05 x 10-5 M
Compound: 8
Growth inhibition of human SKOV3 cells by sulforhodamine B assay
Growth inhibition of human SKOV3 cells by sulforhodamine B assay
[PMID: 19961183]
SN12C GI50
4.26 x 10-2 μM
Compound: 8
Growth inhibition of human SN12C cells by sulforhodamine B assay
Growth inhibition of human SN12C cells by sulforhodamine B assay
[PMID: 19961183]
SNB-19 GI50
4.5 x 10-1 μM
Compound: 8
Growth inhibition of human SNB19 cells by sulforhodamine B assay
Growth inhibition of human SNB19 cells by sulforhodamine B assay
[PMID: 19961183]
SNB-75 GI50
2.98 x 10-5 M
Compound: 8
Growth inhibition of human SNB75 cells by sulforhodamine B assay
Growth inhibition of human SNB75 cells by sulforhodamine B assay
[PMID: 19961183]
SW-620 GI50
6.15 x 10-2 μM
Compound: 8
Growth inhibition of human SW620 cells by sulforhodamine B assay
Growth inhibition of human SW620 cells by sulforhodamine B assay
[PMID: 19961183]
T47D GI50
1.23 μM
Compound: 8
Growth inhibition of human T47D cells by sulforhodamine B assay
Growth inhibition of human T47D cells by sulforhodamine B assay
[PMID: 19961183]
TK-10 GI50
1.82 x 10-5 M
Compound: 8
Growth inhibition of human TK10 cells by sulforhodamine B assay
Growth inhibition of human TK10 cells by sulforhodamine B assay
[PMID: 19961183]
U-251 GI50
5.21 x 10-1 μM
Compound: 8
Growth inhibition of human U251 cells by sulforhodamine B assay
Growth inhibition of human U251 cells by sulforhodamine B assay
[PMID: 19961183]
UACC-257 GI50
1.33 x 10-5 M
Compound: 8
Growth inhibition of human UACC257 cells by sulforhodamine B assay
Growth inhibition of human UACC257 cells by sulforhodamine B assay
[PMID: 19961183]
UACC-62 GI50
1.33 x 10-5 M
Compound: 8
Growth inhibition of human UACC62 cells by sulforhodamine B assay
Growth inhibition of human UACC62 cells by sulforhodamine B assay
[PMID: 19961183]
UO-31 GI50
1.69 x 10-5 M
Compound: 8
Growth inhibition of human UO31 cells by sulforhodamine B assay
Growth inhibition of human UO31 cells by sulforhodamine B assay
[PMID: 19961183]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Liquid

Color

Colorless to light yellow

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

Solution, -20°C, 2 years

Purity & Documentation

Purity: ≥99.0%

References
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Product Name:
GPP78
Cat. No.:
HY-14374
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