TH10785 是 DNA 糖基化酶 1 (OGG1) 的激活剂。TH10785 能与 OGG1 的苯丙氨酸-319 和甘氨酸-42 氨基酸相互作用，提高酶活性，产生 β, δ 裂解酶的酶促功能。TH10785 可在分子结构上控制氮碱介导的催化活性。TH10785 可用于与 DNA 氧化损伤相关的各种疾病和衰老的研究。
| 生物活性 | TH10785 is aDNA glycosylase 1 (OGG1)activator, TH10785 can interact with the phenylalanine-319 and glycine-42amino acidsof OGG1 and increase the enzyme activity, generates β, δ-lyase enzymatic function. TH10785 can control the catalytic activity mediated by a nitrogen base within its molecular structure. TH10785 can be used for the research of various diseases and aging connected with DNA oxidative lesions[1]. |
| IC50& Target | |
体外研究
(In Vitro) | TH10785 (6.25 μM, 30 min) induces a de novo β, δ-elimination in vitro, allowing for AP sites as new substrates[1].
TH10785 (10 μM, 0-2 min) allows OGG1 to increase DNA repair by addressing AP sites[1].
TH10785 (0-20 μM, 72 h) induces OGG1 β, δ-lyase activity shifts cells toward PNKP1 dependence[1].
TH10785 (2 μM) has affinity to OGG1 (KD=5.5 μM) increased when adding an AP site analog containing double-stranded DNA (KD=1.3 μM)[1].
Cell Viability Assay[1] | Cell Line: | U2OS cells | | Concentration: | 0-20 μM | | Incubation Time: | 72 hours | | Result: | Reduced combination with PNKP1 inhibition for TH10785. |
Western Blot Analysis[1] | Cell Line: | U2OS cells | | Concentration: | 0.65 μM; 10 μM | | Incubation Time: | 30 min; 24 h | | Result: | Caused an up-regulation of members of the DDR through β, δ-elimination in combination with PNKP1 inhibition and APE1-independent de novo β, δ-elimination of AP sites by OGG1 in the presence of TH10785. |
RT-PCR[1] | Cell Line: | U2OS cells | | Concentration: | 10 μM | | Incubation Time: | 1 h | | Result: | Decreased oxidative damage in guanine-rich regions of the genome. |
Immunofluorescence[1] | Cell Line: | U2OS OGG1-GFP cells | | Concentration: | 1 μM | | Incubation Time: | 0-2 min | | Result: | Ecruited more OGG1 to laser-damaged sites. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(374.01 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.7401 mL | 18.7007 mL | 37.4014 mL | | 5 mM | 0.7480 mL | 3.7401 mL | 7.4803 mL | | 10 mM | 0.3740 mL | 1.8701 mL | 3.7401 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。-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: ≥ 2.5 mg/mL (9.35 mM); Suspended solution
此方案可获得 ≥ 2.5 mg/mL (9.35 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.35 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.35 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 25.0 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。
|
m.cnreagent.com