SSK1，是一种衰老特异性杀伤化合物，是一种 β-galactosidase 靶向前药，可减轻炎症。SSK1 被溶酶体 β-galactosidase 激活，并通过激活p38 MAPK和诱导细胞凋亡 (apoptosis) 选择性杀死衰老细胞。
| 生物活性 | SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation ofp38 MAPKand induction ofapoptosis[1]. |
体外研究
(In Vitro) | SSK1 (0.5 μM; 12-72 hours) activates the phosphorylation levels of both p38 MAPK and MKK3/MKK6 in senescent cells. SSK1 kills senescent cells through the activation of the p38 MAPK signaling pathway. SSK1 is able to induce mitochondrial DNA damage in senescent cells[1].
SSK1 (0.01-1 μM; 3 days) selectively and potently eliminates β-galactosidase-positive senescent cells within a wide therapeutic window[1].
Cell Proliferation Assay[1] | Cell Line: | Primary mouse fibroblasts | | Concentration: | 0.5 μM | | Incubation Time: | 12 hours, 24 hours, 36 hours, 48 hours, 72 hours | | Result: | Both p38 MAPK and MKK3/MKK6 were activated by phosphorylation in senescent cells. |
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体内研究
(In Vivo) | SSK1 (0.5 mg/kg; i.p.; two days every week; for four weeks) could eliminate senescent cells and decrease senescence-associated markers in lung-injured mice[1].
In aged mice (20-month-old), SSK1 (0.5 mg/kg; 3 days every 2 weeks for 8 weeks) effectively clears senescent cells in different tissues, decreases the senescence- and age-associated gene signatures, attenuates low-grade local and systemic inflammation, and restores physical function[1].
| Animal Model: | Mice (3-6-month-old) were subjected to transtracheal injection of Bleomycin[1] | | Dosage: | 0.5 mg/kg | | Administration: | Intraperitoneally injection; two days every week; for four weeks | | Result: | SSK1 significantly reduced the percentage of SA-β-gal-positive cells in lung by 3.8-fold compared with that in vehicle-treated lung-injured mice |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(253.61 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2681 mL | 6.3403 mL | 12.6805 mL | | 5 mM | 0.2536 mL | 1.2681 mL | 2.5361 mL | | 10 mM | 0.1268 mL | 0.6340 mL | 1.2681 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5 mg/mL (6.34 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.34 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (6.34 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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