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Birinapant

Catalog No. T6007 CAS 1260251-31-7

Synonyms: TL32711

Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.

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

Birinapant, CAS 1260251-31-7

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 193.00
50 mg	In stock	$ 277.00
100 mg	In stock	$ 497.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.59%

Purity: 99.47%

Purity: 98.32%

Purity: 98%

Purity: 97.42%

Purity: 97.08%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
Targets&IC50	XIAP:45 nM(Kd), CIAP1:<1 nM(Kd)
In vitro	Birinapant binds with XIAP and cIAP1 with Kd of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. [1] Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.[2]
In vivo	Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. [2]
Kinase Assay	Fluorescence polarization assay: The binding affinities of compounds to XIAP and cIAP1 are determined using a fluorogenic substrate and are reported as Kd values. Initially, the dissociation constant (Kd) for the fluorescently labeled modified Smac peptide (AbuRPF-K(5-Fam)-NH2; FP pep-tide) is determined using a fixed concentration of peptide (5 nM) and titrating varying concentrations of protein (0.075–5 μM in half log dilutions). The dose–response curves are produced by a nonlinear least squares fit to a single-site binding model using GraphPad Prism, with 5 nM of FP peptide and 50 nM of XIAP used in the assay. Various concentrations of Smac mimetics (100–0.001 μM in half log dilutions) are added to FP peptide:protein binary complex for 15 min at room temperature in 100μL of 0.1 M potassium phosphate buffer, pH 7.5, containing 100 mg/mL bovine c -globulin. Following incubation, the polarization values are measured on a multi-label plate reader using a 485 nm excitation filter and a 520 nm emission filter.
Cell Research	Cells are allowed to attach for 24 hours and subsequently incubated with Birinapant and/or TNF-α for 24 or 72 hours. Then MTS assay is conducted(Only for Reference)

Synonyms	TL32711
Molecular Weight	806.94
Formula	C42H56F2N8O6
CAS No.	1260251-31-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 51 mg/mL (63.2 mM)

DMSO: 93 mg/mL (115.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Allensworth JL, et al. Breast Cancer Res Treat, 2013, 137(2), 359-371. 2. Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794. 3. Bhatt S, Pioso M S, Olesinski E A, et al. Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia[J]. Cancer Cell,. 2020

Citations

1. Bhatt S, Pioso M S, Olesinski E A, et al. Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia. Cancer Cell. 2020, 38(6): 872-890. e6. 2. Olesinski E A, Bhatia K S, Wang C, et al.Acquired Multidrug Resistance in AML Is Caused by Low Apoptotic Priming in Relapsed Myeloblasts.Blood Cancer Discovery.2024: OF1-OF22.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Cuproptosis Compound Library Clinical Compound Library Anti-Colorectal Cancer Compound Library Anti-Infection Compound Library Anti-Ovarian Cancer Compound Library

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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

Birinapant 1260251-31-7 Apoptosis Microbiology/Virology Proteases/Proteasome HIV Protease IAP inhibit Inhibitor TL-32711 HIV Human immunodeficiency virus TL 32711 TL32711 inhibitor

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