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GDC-0152

Catalog No. T6299 CAS 873652-48-3

Synonyms: GDC0152

GDC-0152 is a potent inhibitor of IAPs.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GDC-0152, CAS 873652-48-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 52.00
5 mg	In stock	$ 88.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 230.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 612.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.32%

Purity: 98.23%

Purity: 97.18%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GDC-0152 is a potent inhibitor of IAPs.
Targets&IC50	cIAP2-BIR3:43 nM(Ki), XIAP-BIR2:112 nM(Ki), XIAP-BIR3:28 nM(Ki), MLXBIR3SG:14 nM(Ki), cIAP1-BIR3:17 nM(Ki)
In vitro	GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. The endogenous association of ML-IAP and Smac is effectively also abolished by GDC-0152 in melanoma SK-MEL28 cells. GDC-0152 lead to a decrease in cell viability in the MDA-MB-231 breast cancer cell line, while having no effect on normal human mammary epithelial cells (HMEC). GDC-0152 is found to activate caspases 3 and 7 in a dose- and time-dependent manner. GDC-0152 is shown to induce rapid degradation of cIAP1 in A2058 melanoma cells. It effectively induces degradation of cIAP1 at concentrations as low as 10 nM, consistent with its affinity for cIAP1.
In vivo	GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma−protein binding of GDC-0152 is moderate and comparable among mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) over the range of concentrations investigated (0.1−100 μM); higher plasma−protein binding is observed in rabbits (95−96%). GDC-0152 does not preferentially distribute to red blood cells with blood−plasma partition ratios of 0.6 to 1.1 in all species tested. The pharmacokinetics for GDC-0152 is achieved with a C max of 53.7 μM and AUC of 203.5 h·μM. [1]
Kinase Assay	Fluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued.
Cell Research	MDA-MB-231 breast carcinoma cells and HMECs are treated with the indicated concentrations of GDC-0152. Cell death is assessed using the CellTiter-Glo luminescent cell viability assay 72 h following the start of treatment.(Only for Reference)

Synonyms	GDC0152
Molecular Weight	498.65
Formula	C25H34N6O3S
CAS No.	873652-48-3

Storage

store at low temperture

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 92 mg/mL (184.5 mM)

Ethanol: 92 mg/mL (184.5 mM)

H2O: 3 mg/mL (6.01 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.

Related compound libraries

This product is contained In the following compound libraries：

Cuproptosis Compound Library NO PAINS Compound Library Clinical Compound Library Apoptosis Compound Library Preclinical Compound Library PPI Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GDC-0152 873652-48-3 Apoptosis IAP Inhibitor GDC0152 inhibit GDC 0152 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.