1. Apoptosis Autophagy Metabolic Enzyme/Protease
  2. Apoptosis Autophagy Glutathione S-transferase
  3. NBDHEX

NBDHEX 是一种有效的谷胱甘肽 S-转移酶 P1-1 (GSTP1-1) 抑制剂。 NBDHEX 诱导肿瘤细胞凋亡。NBDHEX 通过抑制 GST 的催化活性,避免抑制剂被特异性泵从细胞中排出,以及破坏 GSTP1-1 和关键信号传导因子之间的相互作用,从而起到抗癌的作用。NBDHEX 也可以作为晚期自噬抑制剂。

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NBDHEX Chemical Structure

NBDHEX Chemical Structure

CAS No. : 787634-60-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥825
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5 mg ¥750
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10 mg ¥1250
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50 mg ¥3700
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100 mg ¥5400
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200 mg   询价  
500 mg   询价  

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor[1][2].

IC50 & Target

Glutathione S-transferase P1-1 (GSTP1-1)[1];
Apoptosis[1];
Autophagy[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
143B IC50
4.08 μM
Compound: NBDHEX
Antiproliferative activity against human 143B cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human 143B cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 33529017]
A549 IC50
2.88 μM
Compound: NBDHEX
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 33529017]
HOS IC50
1.24 μM
Compound: NBDHEX
Antiproliferative activity against human HOS cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HOS cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 33529017]
HUVEC IC50
0.5 μM
Compound: NBDHEX
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33529017]
L02 IC50
1.56 μM
Compound: NBDHEX
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33529017]
U2OS IC50
0.6 μM
Compound: 1, MC2754, NBDHEX
Cytotoxicity against human U2OS cells assessed as cell survival after 48 hrs SRB assay
Cytotoxicity against human U2OS cells assessed as cell survival after 48 hrs SRB assay
[PMID: 25462236]
体外研究
(In Vitro)

NBDHEX (0.05 -20 μM;48 hours;H69和H69AR cells) 对肺癌H69和H69AR细胞具有细胞毒性[2]
NBDHEX (0-5 μM;24 hours;H69AR 细胞) 处理导致 H69AR 细胞系发生剂量依赖性细胞凋亡[2]
NBDHEX (3 μM;1-12 小时;H69AR 细胞) 处理增加 JNK 的磷酸化/c-Jun 在 H69AR 细胞中呈时间依赖性[2]
NBDHEX 处理显示 p38MAPK 磷酸化显著增加,并且还增加H69 细胞中 GSSG 含量随时间变化[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: H69 and H69AR cells
Concentration: 0.05-20 μM
Incubation Time: 48 hours
Result: The dose-response profiles revealed a good cytotoxic activity both in sensitive H69 cell line (LC50 of 2.3 μM) and in its Adriamycin-resistant counterpart H69AR (LC50 of 4.5 μM).

Apoptosis Analysis[2]

Cell Line: H69AR cells
Concentration: 0 μM, 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM
Incubation Time: 24 hours
Result: Resulted in a dose-dependent apoptosis in the H69AR cell line.

Western Blot Analysis[2]

Cell Line: H69AR cells
Concentration: 3 μM
Incubation Time: 1 hour,3 hours, 6 hours, 12 hours
Result: Increased the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion.
体内研究
(In Vivo)

NBDHEX (0.8 -80 mg/kg/天;口服给药;每天;持续 15 天;SCID 雌性小鼠) 处理导致具有统计学意义的肿瘤抑制 (约 70%)[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID female mice (4-5 weeks) injected with Me501cells[3]
Dosage: 0.8 mg/kg/day, 8.0 mg/kg/day or 80 mg/kg/day
Administration: Oral administration; daily; for 15 days
Result: A statistically significant tumour inhibition (approximately 70%) was observed.
分子量

297.33

Formula

C12H15N3O4S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (420.41 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3633 mL 16.8163 mL 33.6327 mL
5 mM 0.6727 mL 3.3633 mL 6.7265 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.00 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.00 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3633 mL 16.8163 mL 33.6327 mL 84.0817 mL
5 mM 0.6727 mL 3.3633 mL 6.7265 mL 16.8163 mL
10 mM 0.3363 mL 1.6816 mL 3.3633 mL 8.4082 mL
15 mM 0.2242 mL 1.1211 mL 2.2422 mL 5.6054 mL
20 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
25 mM 0.1345 mL 0.6727 mL 1.3453 mL 3.3633 mL
30 mM 0.1121 mL 0.5605 mL 1.1211 mL 2.8027 mL
40 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
50 mM 0.0673 mL 0.3363 mL 0.6727 mL 1.6816 mL
60 mM 0.0561 mL 0.2803 mL 0.5605 mL 1.4014 mL
80 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
100 mM 0.0336 mL 0.1682 mL 0.3363 mL 0.8408 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NBDHEX
目录号:
HY-135318
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