2. Apoptosis
    Anti-infection
  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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Solution
10 mM * 1 mL in DMSO USD 128 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 336 In-stock
100 mg USD 600 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 20 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Birinapant purchased from MCE. 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 MCE. 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].

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

    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].

    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[[email protected]]3N(C([[email protected]@H](NC([[email protected]@H](NC)C)=O)CC)=O)C[[email protected]@H](O)C3)=C(C(N4)=C(C[[email protected]]5N(C([[email protected]@H](NC([[email protected]@H](NC)C)=O)CC)=O)C[[email protected]@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 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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    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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