MG 149是一种组蛋白乙酰转移酶（HAT）抑制剂，对Tip60和MOF的IC50值分别为74μM和47μM。
Cas No.:1243583-85-8
Sample solution is provided at 25 µL, 10mM.
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MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively[1].
In vitro, treatment with 2μM MG 149 for 12h prevented H4K16 acetylation in response to DNA damage induced by doxorubicin in serum-deprived A549 and U2OS[2]; Treatment with 100μM MG 149 for 30min significantly prevented UV-induced XPF acetylation in Hela[3]. In the dose range of 0-30μM, MG 149 treatment for 20h inhibited the catalytic activity of TIP60 in wild-type 2D10 cells in a dose-dependent manner and reversed the HIV latent state[4].
In vivo, 1mg/kg MG 149 administered via intraperitoneal injection could relieve HDM-induced Airway Hyperresponsiveness (AHR) and airway inflammation in murine allergic asthma models[5]. MG 149 administered via intraperitoneal injection at a dose of 1.6mg/kg for 14 days blocked the increased glutamate release in ventral hippocampal CA1 (vCA1) after electrical stimulation in dorsomedial prefrontal cortex (dmPFC) of CRS mice[6].
References:
[1] Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.
[2] García-González R, Morejón-García P, Campillo-Marcos I, Salzano M, Lazo PA. VRK1 Phosphorylates Tip60/KAT5 and Is Required for H4K16 Acetylation in Response to DNA Damage. Cancers (Basel). 2020;12(10):2986.
[3] Wang J, He H, Chen B, et al. Acetylation of XPF by TIP60 facilitates XPF-ERCC1 complex assembly and activation. Nat Commun. 2020;11(1):786.
[4] Li Z, Mbonye U, Feng Z, et al. The KAT5-Acetyl-Histone4-Brd4 axis silences HIV-1 transcription and promotes viral latency. PLoS Pathog. 2018;14(4):e1007012.
[5] Liu Y, Du J, Liu X, et al. MG149 inhibits histone acetyltransferase KAT8-mediated IL-33 acetylation to alleviate allergic airway inflammation and airway hyperresponsiveness. Signal Transduct Target Ther. 2021;6(1):321.
[6] Wang Y, Xia M, Lu J, et al. TIP60 mediates stress-induced hypertension via promoting glutamatedmPFC-to-vCA1 release. Clin Exp Hypertens. 2023;45(1):2259130.
MG 149是一种组蛋白乙酰转移酶（HAT）抑制剂，对Tip60和MOF的IC50值分别为74μM和47μM[1]。
体外实验中，2μM MG 149处理12小时，可抑制血清饥饿的A549和U2OS细胞中由doxorubicin诱导的DNA损伤引起的H4K16乙酰化水平[2]。100μM MG 149处理30分钟，可显著抑制HeLa细胞中紫外诱导的XPF乙酰化[3]。在0-30μM的剂量范围内，MG 149处理20小时后，以剂量依赖的方式抑制野生型2D10细胞中TIP60的催化活性，并逆转HIV潜伏状态[4]。
体内实验中，腹腔注射1mg/kg的MG 149可缓解由HDM诱导的小鼠过敏性哮喘模型中的气道高反应和气道炎症[5]。腹腔注射1.6mg/kg的MG 149连续14天，可阻断CRS小鼠背内侧前额叶皮（dmPFC）电刺激后腹侧海马（vCA1）中谷氨酸释放的增加[6]。
| Cell experiment [1]: | |
Cell lines | Serum-deprived A549 and U2OS |
Preparation Method | Cells were cultured in a medium containing 0.5% serum for 48 hours. After treatment with 2μM MG 149 and 10μM C646 for 10 hours, 10μM doxorubicin was added to induce DNA damage, and the acetylation level of H4K16 was measured after 2 hours. |
Reaction Conditions | 2μM; 12h |
Applications | The inhibitor MG 149 that targets Tip60 prevented H4K16 acetylation in response to DNA damage induced by doxorubicin, but this acetylation was not affected by C646 that inhibits p300, in serum-deprived A549 and U2OS cells. |
| Animal experiment [2]: | |
Animal models | Allergic asthma mice modle |
Preparation Method | Mice were challenged for five consecutive days in two weeks with intranasal administration of 35ml (0.7mg/ml PBS) of whole HDM protein extract to construct allergic asthma model. In the HDM+MG 149 group, the anaesthetized mice were pretreated with intraperitoneal injection of MG 149 (1mg/kg) 60 minutes prior to HDM challenge. Control animals received only PBS. |
Dosage form | 1mg/kg; i.p. |
Applications | Administration of MG 149 significantly reduced the airway resistance, decreased total protein levels and total cell numbers in bronchoalveolar lavage fluid, relieved the inflammatory cell infiltration and mucus secretion and reduced collagen deposition around the airways. |
References: | |
| Cas No. | 1243583-85-8 | SDF | |
| 别名 | Tip60 HAT inhibitor | ||
| 化学名 | 2-(4-heptylphenethyl)-6-hydroxybenzoic acid | ||
| Canonical SMILES | CCCCCCCC1=CC=C(CCC2=C(C(O)=O)C(O)=CC=C2)C=C1 | ||
| 分子式 | C22H28O3 | 分子量 | 340.46 |
| 溶解度 | ≥ 114mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9372 mL | 14.686 mL | 29.372 mL |
| 5 mM | 587.4 μL | 2.9372 mL | 5.8744 mL |
| 10 mM | 293.7 μL | 1.4686 mL | 2.9372 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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