2. Apoptosis
  3. IAP
  4. GDC-0152

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.

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CAS No. : 873652-48-3

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10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
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고객리뷰

Based on 14 publication(s) in Google Scholar

GDC-0152 Related Antibodies

Top Publications Citing Use of Products

    GDC-0152 purchased from MedChemExpress. 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 MedChemExpress. 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

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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)
    Cellular Effect
    Cell Line Type Value Description References
    SK-OV-3 EC50
    2.5 nM
    Compound: GDC-0152
    Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 48 hrs by IncuCyte S3 live-cell analysis
    Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 48 hrs by IncuCyte S3 live-cell analysis
    		[PMID: 31095386]
    SK-OV-3 EC50
    3 nM
    Compound: GDC-0152
    Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 24 hrs by IncuCyte S3 live-cell analysis
    Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 24 hrs by IncuCyte S3 live-cell analysis
    		[PMID: 31095386]
    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].

    MedChemExpress (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].

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

    498.64

    화학식

    C25H34N6O3S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    선적

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

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

    DMSO : 50 mg/mL (100.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 몰농도 계산기

    • 농도 희석 계산기

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서

    Purity: 99.70%

    SDS (393 KB)

    COA (254 KB) LCMS (94 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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.0055 mL 10.0273 mL 20.0545 mL 50.1364 mL
    5 mM 0.4011 mL 2.0055 mL 4.0109 mL 10.0273 mL
    10 mM 0.2005 mL 1.0027 mL 2.0055 mL 5.0136 mL
    15 mM 0.1337 mL 0.6685 mL 1.3370 mL 3.3424 mL
    20 mM 0.1003 mL 0.5014 mL 1.0027 mL 2.5068 mL
    25 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0055 mL
    30 mM 0.0668 mL 0.3342 mL 0.6685 mL 1.6712 mL
    40 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2534 mL
    50 mM 0.0401 mL 0.2005 mL 0.4011 mL 1.0027 mL
    60 mM 0.0334 mL 0.1671 mL 0.3342 mL 0.8356 mL
    80 mM 0.0251 mL 0.1253 mL 0.2507 mL 0.6267 mL
    100 mM 0.0201 mL 0.1003 mL 0.2005 mL 0.5014 mL
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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.

    Keywords:

    GDC-0152873652-48-3GDC0152GDC 0152IAPInhibitorinhibitorinhibit

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    상품명:
    GDC-0152
    Cat. No.:
    HY-13638
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    SAFETY DATA SHEET (SDS)

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