2. Apoptosis
  3. IAP
  4. GDC-0152

GDC-0152 

Cat. No.: HY-13638 Purity: 99.67%
COA Handling Instructions

GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.

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

GDC-0152 Chemical Structure

GDC-0152 Chemical Structure

CAS No. : 873652-48-3

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 90 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 90 In-stock
Solid
5 mg USD 106 In-stock
10 mg USD 165 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

GDC-0152 Related Antibodies

Top Publications Citing Use of Products

    GDC-0152 purchased from MCE. Usage Cited in: Sci Signal. 2018 Jul 17;11(539). pii: eaao3964.  [Abstract]

    iBMDM XIAP-knockout cells reconstituted with the indicated IAP protein are treated with TNF (10 ng/mL) alone or in combination with GDC-0152 (200 nM) as indicated for 8 hours, and cellular lysates are assayed by Western blot for caspase-3 cleavage.

    GDC-0152 purchased from MCE. Usage Cited in: J Biol Chem. 2017 Jun 9;292(23):9666-9679.  [Abstract]

    Western blot of lysates from DC2.4 Neg, XIAP-G1, and XIAP-G2 cell lines stimulated with TNF (10 ng/uL), GDC-0152 (2 μM), and zVAD (20 μM, TGZ) for 0, 2, or 4 hours in the presence (+) or absence (-) of nec-1 (20 μM). Representative blots from three independent replicates.

    View All IAP Isoform Specific Products:

    View All Isoforms
    cIAP cIAP-1 cIAP-2 XIAP

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.

    IC50 & Target

    Ki: 28 nM (XIAP BIR3), 14 nM (MLIAP-BIR3), 17 nM (cIAP1-BIR3), 43 nM (cIAP2-BIR3)
    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. In melanoma SK-MEL28 cells, the endogenous association of ML-IAP and Smac is also effectively abolished by GDC-0152. GDC-0152 leads 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[1].

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

    GDC-0152 Related Antibodies
    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 ranging from 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    498.64

    Appearance

    Solid

    Formula

    C25H34N6O3S
    CAS No.
    SMILES

    O=C(N1[C@H](C(NC2=C(C3=CC=CC=C3)N=NS2)=O)CCC1)[C@H](C4CCCCC4)NC([C@H](C)NC)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    Ethanol : 50 mg/mL (100.27 mM; Need ultrasonic)

    DMSO : 50 mg/mL (100.27 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0055 mL 10.0273 mL 20.0545 mL
    5 mM 0.4011 mL 2.0055 mL 4.0109 mL
    10 mM 0.2005 mL 1.0027 mL 2.0055 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.67%

    COA (254 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Detached cells are washed with phosphate-buffered saline (PBS) and are resuspended in assay media (MDA-MB-231 cells: RPMI1640 supplemented with 10% fetal bovine serum and 2 mM L-glutamine [GlutaMAX-1]) or culture media (HMECs: MEBM® with MEGM SingleQuots®). Cells are placed in tissue culture-treated, white-wall or black-wall, clear-bottom, 96-well plates at 1×104 cells/well in a volume of 50 μL. The plates are incubated at 37°C and 5% CO2 overnight, the media is removed, and GDC-0152 or it's enantiomer are added in assay media. Cells cultured in white-wall, clear-bottom plates are incubated at 37°C and 5% CO2 for 3 days before cell viability is measured using the CellTiter-Glo® luminescent cell viability assay kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Cells are resuspended in PBS and the cell suspension is mixed 1:1 with Matrigel. The cells (1.5×107) are then implanted subcutaneously into the right flank of 130 female nude mice aged 6-8 weeks. Tumor volumes are calculated. Ten mice with the appropriate mean tumor volume are assigned randomLy to each of six groups. The mean tumor volume±the standard error of the mean (SEM) for all six groups is 168±3 mm3 at the initiation of treatment (Day 0). Mice are dosed 1 or vehicle (PBS) by oral gavage with a dose volume of 4.0 mL/kg. The mice are observed on each day of the study, and tumor volumes and body weights are measured twice each week. Percent tumor growth inhibition is calculated using the formula %TGI=100× (1- Tumor Volumedose/Tumor Volumevehicle).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    GDC-0152 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    GDC-0152873652-48-3GDC0152GDC 0152IAPInhibitorinhibitorinhibit

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