Kelch-like ECH-associated protein 1 (Keap1), leading to activation of nuclear factor erythroid 2-related factor 2 (Nrf2) [4]
AMP-activated protein kinase (AMPK) [4]
HDAC; Bax; Caspase-3

- 在HT29人结肠癌细胞中，莱菔硫烷以剂量依赖方式诱导G2/M期细胞周期阻滞和凋亡。它降低cyclin B1和cdc2的表达，增加p21的表达。凋亡与细胞色素c从线粒体释放、caspases-3和-9的激活以及多聚（ADP-核糖）聚合酶（PARP）的切割相关[1]
- 在大鼠H9c2细胞中，莱菔硫烷可防止阿霉素诱导的氧化应激和细胞死亡。它提高超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和谷胱甘肽过氧化物酶（GPx）的活性，减少活性氧（ROS）生成和丙二醛（MDA）水平，并通过上调Bcl-2、下调Bax和切割的caspase-3来抑制阿霉素诱导的凋亡[2]
- 在多种癌细胞系（包括乳腺癌、结肠癌和肺癌细胞）中，莱菔硫烷通过抑制细胞增殖和诱导凋亡发挥抗癌活性。它还抑制I相酶（如细胞色素P450 1A1）的活性，并诱导II相解毒酶（如醌还原酶）[3]
- 在高糖条件下的胰腺癌细胞中，莱菔硫烷激活Nrf2，进而抑制细胞增殖、迁移和侵袭，并促进凋亡。这种作用通过AMPK依赖的信号通路介导，因为莱菔硫烷增加AMPK的磷酸化，且该作用可被AMPK抑制剂逆转[4]
萝卜硫素以剂量依赖性方式导致细胞周期停滞并最终导致细胞死亡。细胞周期蛋白 A 和 B1 的较高表达与萝卜硫素诱导的细胞周期停止有关。萝卜硫素会导致细胞凋亡，这是细胞死亡的过程。萝卜硫素对分化的 CaCo2 细胞危害较小，可减缓静止结肠癌细胞 (HT29) 的生长恢复，同时还会降低其细胞活力 [1]。萝卜硫素预处理 H9c2 大鼠成肌细胞，减少了凋亡细胞的数量和促凋亡蛋白的表达（Bax、caspase-3 和细胞色素 c），以及阿霉素引起的线粒体膜电位的增加。此外，萝卜硫素通过增加血红素加氧酶-1 的 mRNA 和蛋白质表达来降低阿霉素诱导的线粒体中活性氧（ROS，由 MitoSOX Red 试剂测定）水平 [2]。

在小鼠中，莱菔硫烷通过抑制致癌物诱导的结肠癌前病变的形成而表现出抗癌活性。它还在多种组织（包括肝脏、结肠和小肠）中诱导II相解毒酶[3]
萝卜硫素可减少用单剂量 9,10-二甲基-1,2-苯并蒽治疗的 Sprague-Dawley 大鼠的乳腺肿瘤生长。萝卜硫素的施用可降低雌性 Sprague-Dawley 大鼠单剂量 DMBA 产生的乳腺肿瘤的发生率、多重性和重量，并减缓其进展 [3]。

- 对于HT29结肠癌细胞：将细胞在培养基中培养，用不同浓度（0-40μM）的莱菔硫烷处理不同时间。通过碘化丙啶染色和流式细胞术进行细胞周期分析。通过膜联蛋白V-FITC/PI染色、TUNEL测定和caspase活性检测评估凋亡。采用蛋白质印迹分析检测细胞周期相关蛋白（cyclin B1、cdc2、p21）和凋亡标志物（细胞色素c、caspases-3/-9、PARP）的表达[1]
- 对于H9c2细胞：在阿霉素暴露前，用莱菔硫烷（0-5μM）预处理细胞。使用相应的检测试剂盒测量氧化应激标志物（ROS、MDA、SOD、CAT、GPx）。通过MTT测定法确定细胞活力，并通过蛋白质印迹分析Bcl-2、Bax和切割的caspase-3来分析凋亡[2]
- 对于胰腺癌细胞：将细胞在高糖条件下培养并经莱菔硫烷处理。通过CCK-8测定评估细胞增殖，通过transwell实验评估迁移和侵袭，通过流式细胞术评估凋亡。采用蛋白质印迹检测Nrf2、HO-1、NQO1、p-AMPK等相关蛋白。通过免疫荧光分析Nrf2的核转位[4]

Mice were administered Sulforaphane via oral gavage at a dose of 200 μmol/kg body weight. After treatment, mice were sacrificed, and various tissues (liver, colon, small intestine) were collected. The activity of phase II detoxifying enzymes (quinone reductase) was measured in tissue homogenates. For carcinogen-induced preneoplastic lesion models, mice were treated with carcinogens and Sulforaphane concurrently, and the number of lesions was counted histologically [3]

[1]. Sulforaphane, a naturally occurring isothiocyanate, induces cell cycle arrest and apoptosis in HT29 human colon cancer cells. Cancer Res. 2000 Mar 1;60(5):1426-33.
[2]. Sulforaphane prevents doxorubicin-induced oxidative stress and cell death in rat H9c2 cells. Int J Mol Med. 2015 Jul;36(1):53-64.
[3]. Anticarcinogenic activities of sulforaphane and structurally related synthetic norbornylisothiocyanates. Proc Natl Acad Sci U S A. 1994 Apr 12;91(8):3147-50.
[4]. Activation of Nrf2 by Sulforaphane Inhibits High Glucose-Induced Progression of PancreaticCancer via AMPK Dependent Signaling. ell Physiol Biochem. 2018;50(3):1201-1215

- Sulforaphane is a naturally occurring isothiocyanate found in cruciferous vegetables. Its anticarcinogenic activity is partly attributed to the induction of phase II detoxifying enzymes, which enhance the detoxification of carcinogens, and the inhibition of phase I enzymes, which reduce the activation of procarcinogens [3]
- In colon cancer cells, the induction of apoptosis by Sulforaphane involves the mitochondrial pathway, characterized by cytochrome c release and caspase activation [1]
- The protective effect of Sulforaphane against doxorubicin-induced cell damage is related to its antioxidant properties, reducing oxidative stress and inhibiting apoptotic pathways [2]
Sulforaphane is an isothiocyanate having a 4-(methylsulfinyl)butyl group attached to the nitrogen. It has a role as an antineoplastic agent, a plant metabolite, an antioxidant and an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a sulfoxide and an isothiocyanate.
Sulforaphane is under investigation for the treatment of Autism Spectrum Disorder. It is a naturally occurring isothiocyanate found in high concentration in a variety of broccoli.
Sulforaphane has been reported in Brassica oleracea, Brassica oleracea var. sabauda, and other organisms with data available.
Sulforaphane is a naturally-occurring phytochemical belonging to the class of isothiocyanates. As the aglycone metabolite of glucosinolate glucoraphanin (sulforaphane glucosinolate), sulforaphane acts as an antioxidant and potent stimulator of endogenous detoxifying enzymes. This agent displays anticarcinogenic properties due to its ability to induce phase II detoxification enzymes, such as glutathione S-transferase and quinone reductase, thereby providing protection against certain carcinogens and toxic, reactive oxygen species. Broccoli sprouts contain large amounts of sulforaphane, which is also found in other cruciferous vegetables including cabbage and kale. (NCI04)

C6H11NOS2

177.3

177.028

C, 40.65; H, 6.25; N, 7.90; O, 9.02; S, 36.17

4478-93-7

142825-10-3 (R-isomer); 155320-20-0 (S-isomer); 4478-93-7 (racemic);

5350

Colorless to light yellow liquid

1.2±0.1 g/cm3

368.2±25.0 °C at 760 mmHg

176.5±23.2 °C

0.0±0.8 mmHg at 25°C

1.567

0.23

80.73

0

4

5

10

152

0

O=S(CCCCN=C=S)C

SUVMJBTUFCVSAD-UHFFFAOYSA-N

InChI=1S/C6H11NOS2/c1-10(8)5-3-2-4-7-6-9/h2-5H2,1H3

1-isothiocyanato-4-(methylsulfinyl)butane

Sulforafan; Sulforaphane; BroccoPhane; sulforaphane; 4478-93-7; 1-Isothiocyanato-4-(methylsulfinyl)butane; Sulforafan; 1-isothiocyanato-4-methylsulfinylbutane; Sulphoraphane; Butane, 1-isothiocyanato-4-(methylsulfinyl)-; CHEBI:47807; Detoxophane; Broccoli sprout extracts; 4-methyl-sulfinybutyl isothiocyanatel

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。  (2). 该产品在溶液状态不稳定，请现配现用。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 62.5 mg/mL (~352.53 mM)
H2O : ~50 mg/mL (~282.02 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (14.10 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (14.10 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (14.10 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 10 mg/mL (56.40 mM) in 30 % SBE-β-CD (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。