Nicotinamide (Synonyms: 烟酰an; Niacinamide; Nicotinic acid amide)
Nicotinamide 是wei生素 B3 或烟suan的一种形式,可抑制 SIRT2 的体外活性,其 EC50 值为 2 μM。 Nicotinamide 可抑制 90% 的黑色素瘤细胞数量,并增加细胞内 NAD+、ATP、ROS 水平。Nicotinamide 抑制黑色素瘤小鼠的肿瘤生长并提高生存率,可用于黑色素瘤等皮肤ai相关的研究。
生物活性
Nicotinamide is a form of vitamin B3 or niacin that inhibits sirtuin 2 (SIRT2) activity in vitro, with an EC50 of 2 μM. Nicotinamide inhibits up to 90% melanoma cell number and increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma[1].
体外研究(In Vitro)
Nicotinamide (0-50 mM, 24/48 h ) reduces cell number in a time-dependent and dose-dependent manner in A375 and SK-MEL-28 cells[1].
Nicotinamide (10-50 mM, 24 h ) makes A375 cells undergo accumulation in G1 phase, reduction in S phase, and increase inthe sub-G1 (apoptosis) phase[1].
Nicotinamide (1-50 mM, 6 h ) increases NAD+, ATP and ROS levels in A375 and SK-MEL-28 cells[1].
Nicotinamide (0.01-20 mM, 1 h) inhibits purified SIRT2 enzymatic activity in vitro with an EC50 of 2 μM[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line: | A375, SK-MEL-28, mouse B16-F10 cell |
Concentration: | 0, 1, 20, 50 mM |
Incubation Time: | |
Result: | 24 h, 48 h |
体内研究(In Vivo)
Nicotinamide (Intraperitoneal injection, 1500 and 1800 mg/Kg, 5 days per week) inhibits tumor growth in murine metastatic melanoma model[1].
Nicotinamide (Intraperitoneal injection, 1800 mg/Kg, once a day, murine metastatic melanoma model) affects IFN-γ (a key mediator of cell-mediated anti-tumor immunity), increases the plasma levels of eotaxin and IL-5, reduces the plasma levels of IL-3, IL-12, RANTES and IL-10[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | C57BL/6 mice (subcutaneous injected with B16-F10 cells)[1] |
Dosage: | 1000, 1500, 1800 mg/Kg. |
Administration: | Intraperitoneal injection, 5 days per week (followed by 2-day rest) or once a day. |
Result: | Inhibited tumor growth at 1500 and 1800 mg/Kg, and had no effect on the body weight. Increased the frequency of IFN-γ producing cells and modulated the protein levels of cytokines and chemokines in the plasma of tumor-bearing mice. |
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04910061 | Seneque SA|Dicentra Inc.|LGD | August 5, 2021 | Not Applicable | |
NCT05258474 | University Hospital Schleswig-Holstein | December 4, 2020 | Phase 1 | |
NCT05194397 | Children´s Hospital of Philadelphia|National Institutes of Health (NIH)|City of Hope Medical Center|St. Jude Children´s Research Hospital|National Cancer Institute (NCI)|University of Pennsylvania | November 18, 2022 | Phase 2 |
分子量:122.12
性状:Solid
Formula:C6H6N2O
CAS 号:98-92-0
中文名称:烟酰an
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro:
DMSO : 50 mg/mL (409.43 mM; Need ultrasonic)
H2O : ≥ 50 mg/mL (409.43 mM)
* "≥" means soluble, but saturation unknown.
浓度溶剂体积质量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 8.1887 mL | 40.9433 mL | 81.8867 mL |
5 mM | 1.6377 mL | 8.1887 mL | 16.3773 mL |
10 mM | 0.8189 mL | 4.0943 mL | 8.1887 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°C, 6 months; -20°C, 1 month (protect from light)。-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。
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: PBS
Solubility: 100 mg/mL (818.87 mM); Clear solution; Need ultrasonic
- 2.
请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
- 3.
请依序添加每种溶剂: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
- 4.
请依序添加每种溶剂: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
参考文献
[1]. [1] Francesca Scatozza, et al. Nicotinamide inhibits melanoma in vitro and in vivo. J Exp Clin Cancer Res. 2020 Oct 7;39(1):211. [Content Brief]
注:产品仅用于科研