受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C62H84N14O6 |
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分子量 | 1121.42 | CAS No. | 957135-43-2 | |
Solubility (25°C)* | 体外 | DMSO | 50 mg/mL (44.58 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression. |
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製品説明 | SM-164 is a potent, non-peptide, cell-permeable antagonist of XIAP that targets both the BIR2 and BIR3 domains with IC50 of 1.39 nM. SM-164 induces apoptosis and tumor regression. |
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in vitro | SM-164 binds to XIAP containing both BIR domains with IC50 of 1.39 nM, being 300 and 7000 times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in the HL-60 leukemia cell line. [1] SM-164 induces caspase-8– and caspase-3–dependent apoptosis in cancer cells. SM-164 induces TNFα-dependent apoptosis and cIAP-1 degradation. [2] SM-164 is highly synergistic with TRAIL in vitro in both TRAIL-sensitive and TRAIL-resistant cancer cell lines of breast, prostate, and colon cancer. SM-164 enhances TRAIL-induced apoptosis in cancer cells through amplification of the caspase-8–mediated extrinsic apoptosis pathway [3] |
in vivo | SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. [2] SM-164 induces cIAP1 degradation in tumor tissues and dramatically enhances the in vivoantitumor activity of TRAIL, and the combination of SM-164 and TRAIL achieves tumor regression without toxicity to animals. [3] |
特徴 | The potency of bivalent SM-164 in binding, functional, and cellular assays is 2−3 orders of magnitude higher than its corresponding monovalent Smac mimetics. |
キナーゼアッセイ | Binding assays. | |
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The FP-based assay for XIAP BIR3 protein is described. Briefly, 5-carboxyfluorescein is coupled to the lysine side chain of a mutated Smac peptide with the sequence and this fluorescently tagged peptide (named SM5F) is used as the fluorescent tracer in FP-based binding assay to XIAP BIR3. The Kd value of this fluorescent tracer is determined to be 17.9 nM to XIAP BIR3. In competitive binding experiments, a tested compound is incubated with 30 nM ofXIAP BIR3 protein and 5 nM of SM5F in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/ml bovine gamma globulin; 0.02 % sodium azide). The Kd value of SM5F to cIAP-1 BIR3 protein is determined to be 4.1 nM. In competitive binding experiments, 10 nM of cIAP-1 BIR3 protein and 2 nM of SM5F tracer are used. The Kd value of SM5F to cIAP-2 BIR3 protein is determined to be 6.6 nM. In competitive binding experiments, 25 nM of cIAP-2 BIR3 proteinand 2 nM of SM5F tracer are used. To determine the binding affinities of Smac mimetics to XIAP containing both BIR2 and BIR3 domains, an FP-based competitive binding assay is established using a bivalentfluorescently tagged tracer, named Smac-1F. The Kd value of the bivalent tagged tracer to XIAP containing BIR2 and BIR3 domains is determined to be 2.3 nM. In competitive binding experiments, a tested compound is incubated with 3 nM of XIAP protein containing both BIR2 and BIR3 domain (residues 120-356) and 1 nM of in the sameassay buffer. | ||
細胞アッセイ | 細胞株 | HT-29 cells |
濃度 | 1 μM | |
反応時間 | 6 or 12 h | |
実験の流れ | Cells pre-treated with HG (5 μM) for 30 min were treatment with SM-164 (1 μM) for 6 or 12 h. |
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動物実験 | 動物モデル | MDA-MB-231 xenografted SCID mice |
投薬量 | 1 and 5 mg/kg | |
投与方法 | i.v. |
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CSFV restricts necroptosis to sustain infection by inducing autophagy/mitophagy-targeted degradation of RIPK3 [ Microbiol Spectr, 2024, 12(1):e0275823] | PubMed: 38100396 |
Uptake-independent killing of macrophages by extracellular Mycobacterium tuberculosis aggregates [ EMBO J, 2023, e113490.] | PubMed: 36920246 |
TRAF2/3 deficient B cells resist DNA damage-induced apoptosis via NF-κB2/XIAP/cIAP2 axis and IAP antagonist sensitizes mutant lymphomas to chemotherapeutic drugs [ Cell Death Dis, 2023, 14(9):599] | PubMed: 37679334 |
TRAF2/3 deficient B cells resist DNA damage-induced apoptosis via NF-κB2/XIAP/cIAP2 axis and IAP antagonist sensitizes mutant lymphomas to chemotherapeutic drugs [ Cell Death Dis, 2023, 14(9):599] | PubMed: 37679334 |
Epithelial Gab1 calibrates RIPK3-dependent necroptosis to prevent intestinal inflammation [ JCI Insight, 2023, 8(6)e162701] | PubMed: 36795486 |
Mycoplasma hyorhinis infection promotes TNF-α signaling and SMAC mimetic-mediated apoptosis in human prostate cancer [ Heliyon, 2023, 9(10):e20655] | PubMed: 37867861 |
Mycoplasma hyorhinis infection promotes TNF-α signaling and SMAC mimetic-mediated apoptosis in human prostate cancer [ Heliyon, 2023, 9(10):e20655] | PubMed: 37867861 |
Salt-inducible kinases inhibitor HG-9-91-01 targets RIPK3 kinase activity to alleviate necroptosis-mediated inflammatory injury [ Cell Death Dis, 2022, 13(2):188] | PubMed: 35217652 |
Protection of Quiescence and Longevity of IgG Memory B Cells by Mitochondrial Autophagy [ J Immunol, 2022, 208(5):1085-1098] | PubMed: 35101890 |
Protection of Quiescence and Longevity of IgG Memory B Cells by Mitochondrial Autophagy [ J Immunol, 2022, 208(5):1085-1098] | PubMed: 35101890 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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