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  3. IAP Apoptosis HIV
  4. Birinapant

Birinapant  (Synonyms: TL32711)

Cat. No.: HY-16591 Purity: 99.70%
COA Handling Instructions

Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

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

Birinapant Chemical Structure

Birinapant Chemical Structure

CAS No. : 1260251-31-7

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10 mM * 1 mL in DMSO
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10 mg USD 144 In-stock
50 mg USD 336 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Birinapant Related Antibodies

Top Publications Citing Use of Products

    Birinapant purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jul 25;178(3):585-599.e15.  [Abstract]

    Western blot analysis of polyclonal pools of sgCtrl or sgTRAF2-expressing SK-MEL-23 melanoma cells in the presence or absence of Birinapant, and upon coculture with MART-1 T cell for indicated amounts of time.

    Birinapant purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2018 Sep 19;9:2022.  [Abstract]

    ACH-2 cells are exposed to Birinapant (50 nM) in the presence or absence of PEP005 (5 nM), with TNF-α (10 ng/ml) co-treatment for 24 h, and cell lysates are used for WB analysis.

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    cIAP cIAP-1 cIAP-2 XIAP

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

    IC50 & Target

    Kd: 45 nM (XIAP), <1 nM (cIAP1)[1]
    In Vitro

    Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner[1].
    ? Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis[1].
    ? Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation[1].

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

    Birinapant Related Antibodies

    Cell Viability Assay[1]

    Cell Line: TRAIL-resistant SUM190 IBC cells
    Concentration: 30, 100, 300, 1000, 10000 nM
    Incubation Time: 24 hours
    Result: Significantly decreased the viability of SUM190 cells in a dose-dependent manner.

    Western Blot Analysis[1]

    Cell Line: SUM190 cells
    Concentration: 30, 300, 1000 nM
    Incubation Time: 4 hours
    Result: Showed a significant decrease in cIAP1 levels and enhanced PARP cleavage.
    In Vivo

    Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models[2].

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

    Animal Model: Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma)[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; every third day (*5)
    Result: Resulted in inhibition of tumor growth.
    Clinical Trial
    Molecular Weight

    806.94

    Appearance

    Solid

    Formula

    C42H56F2N8O6
    CAS No.
    SMILES

    FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (154.91 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2392 mL 6.1962 mL 12.3925 mL
    5 mM 0.2478 mL 1.2392 mL 2.4785 mL
    10 mM 0.1239 mL 0.6196 mL 1.2392 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: ≥ 2.08 mg/mL (2.58 mM); Clear solution

    • 2.

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

      Solubility: 2.08 mg/mL (2.58 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (2.58 mM); Clear solution

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

    Purity: 99.70%

    COA (256 KB) HNMR (221 KB) RP-HPLC (114 KB) LCMS (114 KB)

    Handling Instructions (2659 KB)
    References
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    Birinapant 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:

    Birinapant1260251-31-7TL32711TL 32711TL-32711IAPApoptosisHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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