3-TYP |
Catalog No.GC19013
One-Click Copy Product Info
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3-TYP is an orally active SIRT3 inhibitor (IC50=16nM) and also inhibits SIRT1 (IC50=88nM) and SIRT2 (IC50=92nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120241-79-4
Sample solution is provided at 25 µL, 10mM.
3-TYP is an orally active SIRT3 inhibitor (IC50=16nM) and also inhibits SIRT1 (IC50=88nM) and SIRT2 (IC50=92nM). 3-TYP selectively inhibits the deacetylase function of SIRT3, leading to mitochondrial protein hyperacetylation. 3-TYP thereby regulates oxidative phosphorylation and increases reactive oxygen species levels in cancer cells and primary hepatocytes. 3-TYP can be used in research on metabolic diseases, aging and tumor metabolism[1-4].
In vitro, treatment of MV4-11 cells with 50μM 3-TYP for 48 hours increased SOD2 acetylation levels in the cells[5]. During 6 hours of reoxygenation after 24 hours of hypoxia, treatment of H9c2 cells with 50μM 3-TYP aggravated hypoxia-reoxygenation-induced decline in mitochondrial respiration capacity and caused abnormal mitophagy[6]. During 2 hours of reoxygenation after 10 hours of hypoxia, treatment of H9c2 cells with 1μM 3-TYP aggravated cell morphological damage, enhanced hypoxia/reoxygenation-induced inhibition of cell proliferation, increased apoptosis rate, increased caspase-3 and Bax protein expression and decreased Bcl-2 expression, and elevated LDH release in culture medium[7].
In vivo, intraperitoneal injection of 50mg/kg 3-TYP into ACE2 knockout mice combined with 1g/kg β-aminopropionitrile fumarate in drinking water once every two days for 4 consecutive weeks increased mortality and incidence of thoracic aortic dissection, enlarged the maximum internal diameter of the thoracic aorta, worsened thoracic aortic histological injury and destroyed elastic fibers [8]. A single intraperitoneal injection of 50mg/kg 3-TYP into C57BL/6J mice 2 hours before thioacetamide (300mg/kg) injection aggravated liver tissue necrosis and inflammatory cell infiltration, increased serum ALT and AST levels, reduced 24-hour survival rate, decreased liver GSH content and increased MDA content [9]. Daily intraperitoneal injection of 20mg/kg 3-TYP into APP/PS1 mice combined with intragastric administration of 20mg/kg/day honokiol for 5 consecutive days eliminated the cognitive improvement effect of honokiol, restored prolonged escape latency and platform crossing latency and reduced platform crossing frequency, and abolished the reduction of Aβ1-42 plaque deposition in hippocampus and cortex induced by honokiol [10].
References:
[1] Song S, Yang M, Li J, et al. Z. SIRT3 mediates CPT2 delactylation to enhance mitochondrial function and proliferation in goat granulosa cells. J Anim Sci Biotechnol. 2025 Jul 17;16(1):101.
[2] Huang X, Gou H, Xie J, et al. Sirt3 Rescues Porphyromonas gingivalis-Impaired Cementogenesis via SOD2 Deacetylation. Cell Prolif. 2025 Sep;58(9):e70022.
[3] Zhu Z, Wang Y, Chen J, et al. 3-TYP protects against heart failure with preserved ejection fraction by inhibiting Sirtuin 3. J Mol Histol. 2025 Oct 23;56(6):357.
[4] Zeng Y, Zhang Y, Cui Z, et al. The Selective SIRT3 Inhibitor 3-TYP Represses Primary Myeloma Growth by Reducing c-Myc Stability. Chem Res Toxicol. 2024.
[5] Ma J, Liu B, Yu D, et al. SIRT3 deacetylase activity confers chemoresistance in AML via regulation of mitochondrial oxidative phosphorylation. Br J Haematol. 2019;187(1):49-64.
[6] Kranrod JW, Valencia R, Heidari M, et al. Establishing a direct interaction between the 19,20-EDP analog SA-22 and SIRT3: impact on cardiac mitochondrial homeostasis. Front Pharmacol. 2026 Jun 2;17:1805965.
[7] Wu H, Liu Y, Hao Y, et al. Lycium barbarum polysaccharide protects cardiomyocytes from hypoxia/reoxygenation injury via activation of SIRT3/CypD signaling. Ann Transl Med. 2023 Jan 31;11(2):72.
[8] Jiang L, Lu L, Xue C, et al. ACE2 deficiency inhibits thoracic aortic dissection by enhancing SIRT3 mediated inhibition of inflammation and VSCMs phenotypic switch. Mol Med. 2024 Sep 19;30(1):154.
[9] Shi C, Jiao F, Wang Y, et al. SIRT3 inhibitor 3-TYP exacerbates thioacetamide-induced hepatic injury in mice. Front Physiol. 2022 Jul 18;13:915193.
[10] Li H, Sun J, Wu Y, et al. Honokiol relieves hippocampal neuronal damage in Alzheimer's disease by activating the SIRT3-mediated mitochondrial autophagy. CNS Neurosci Ther. 2024;30:e14878.
| Cell experiment [1]: | |
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Cell lines |
H9c2 cells (rat cardiac myoblast cell line) |
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Preparation Method |
H9c2 cells were cultured in DMEM with 10% FBS at 37°C, 5% CO2. H9c2 cells were pre-cultured with 2.0μg/mL Lycium barbarum polysaccharide for 48 hours, then subjected to hypoxia for 10 hours followed by reoxygenation for 2 hours, with 1μM 3-TYP added during H/R to inhibit SIRT3; cell morphology was observed by light microscopy, proliferation was assessed by CCK-8 and EdU assays, apoptosis was assessed by flow cytometry, CypD lysine-166 acetylation was determined by co-immunoprecipitation and Western blot, LDH release was measured by ELISA, and Na+-K+-ATPase activity, Ca2+-ATPase activity and NO levels were measured. |
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Reaction Conditions |
1μM; during 10h hypoxia + 2h reoxygenation |
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Applications |
3-TYP aggravated H/R-induced morphological damage, enhanced H/R-induced inhibition of cell proliferation, increased H/R-induced apoptosis rate, restored CypD acetylation elevated by H/R, blocked LBP-induced CypD deacetylation, increased LDH release. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice and ACE2 knockout (ACE2-/-) mice |
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Preparation Method |
Three-week-old male C57BL/6J mice and ACE2-/- mice were fed 1g/kg β-aminopropionitrile fumarate (BAPN) in drinking water for 4 weeks; 3-TYP was intraperitoneally injected at 50mg/kg once every 2 days during the BAPN treatment period. Survival, thoracic aortic maximum internal diameter (transthoracic ultrasound), macroscopic dissection incidence, H&E and EVG histology, immunohistochemistry (CD68, OPN, SM22α, SIRT3), and Western blot (MMP2, MMP9, IL-1β, IL-6, TNF-α, NLRP3, SIRT3, Ac-SOD2) of thoracic aorta were assessed at endpoint. |
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Dosage form |
50mg/kg/time; i.p.; once every 2 days |
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Applications |
3-TYP increased mortality and incidence of thoracic aortic dissection, enlarged maximal internal diameter of thoracic aorta, worsened H&E and EVG histological injury with degraded elastic fibers, increased MMP2 and MMP9 protein expression, elevated IL-1β, IL-6, TNF-α and NLRP3 expression, upregulated OPN and downregulated SM22α in thoracic aorta, reduced SIRT3 expression and increased Ac-SOD2 expression in BAPN-treated wild-type and ACE2-/- mice, and reversed the protective effects of ACE2 deficiency against BAPN-induced aortic injury and VSMC phenotypic switch. |
References: [1] Wu H, Liu Y, Hao Y, et al. Lycium barbarum polysaccharide protects cardiomyocytes from hypoxia/reoxygenation injury via activation of SIRT3/CypD signaling. Ann Transl Med. 2023 Jan 31;11(2):72. [2] Jiang L, Lu L, Xue C, et al. ACE2 deficiency inhibits thoracic aortic dissection by enhancing SIRT3 mediated inhibition of inflammation and VSCMs phenotypic switch. Mol Med. 2024 Sep 19;30(1):154. | |
| Cas No. | 120241-79-4 | SDF | |
| Canonical SMILES | C1(C2=CN=NN2)=CC=CN=C1 | ||
| Formula | C7H6N4 | M.Wt | 146.15 |
| Solubility | DMSO : 100 mg/mL (684.23 mM);Ethanol : 16.67 mg/mL (114.06 mM) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.8423 mL | 34.2114 mL | 68.4229 mL |
| 5 mM | 1.3685 mL | 6.8423 mL | 13.6846 mL |
| 10 mM | 684.2 μL | 3.4211 mL | 6.8423 mL |
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)