2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. MMP Apoptosis Interleukin Related TNF Receptor Caspase
  4. TMI-1

TMI-1  (Synonyms: WAY-171318)

目录号: HY-101448 纯度: 99.59%
COA 产品使用指南 技术支持

TMI-1 (WAY-171318) 是可口服的肿瘤坏死因子转换酶 (TACE) 抑制剂 (IC50: 8.4 nM)，也是 ADAM-TS-4、ADAM-17 及多种 MMPs 的有效抑制剂。TMI-1 能显著抑制 TNF-α 的分泌，减轻小鼠胶原诱导关节炎。TMI-1 抑制肿瘤增殖，通过 Caspase 依赖途径诱导凋亡。TMI-1 还逆转 TRPV1 上调并降低神经细胞内炎症因子 (TNF-α、IL-1β、IL-6) 水平，保护免受紫杉醇引起的神经毒性。TMI-1 导致促动脉粥样硬化脂蛋白谱变化，但不影响早期病变进展。

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TMI-1 Chemical Structure

TMI-1 Chemical Structure

CAS No. : 287403-39-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1100
In-stock
5 mg ￥1000
In-stock
10 mg ￥1750
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

TMI-1 相关抗体

Top Publications Citing Use of Products

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions[1][2][3][4].

IC50 & Target

IL-6

 

IL-1β

 

MMP-1

6.6 nM (IC50)

MMP-2

4.7 nM (IC50)

MMP-7

26 nM (IC50)

MMP-14

26 nM (IC50)

MMP-9

12 nM (IC50)

MMP-13

3 nM (IC50)

TACE

8.8 nM (IC50)

ADAM17

 

ADAM-TS-4

100 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
8 nM
Compound: 6
Inhibition of human TACE expressed in CHO cells by FRET assay
Inhibition of human TACE expressed in CHO cells by FRET assay
[PMID: 17606376]
体外研究
(In Vitro)

TMI-1 在小鼠单核细胞 Raw 中，抑制 TNF-α 分泌，IC50 为 40 nM，在人单核细胞 THP-1 中，IC50 为 200 nM，在原代人单核细胞系的 IC50 为 190 nM，在人全血中 IC50 为 300 nM[1]。
TMI-1 抑制人全血中TNFR Ⅱ 的脱落，IC50 为 0.72 μM[1]。
TMI-1 (0-20 μM，5 days) 剂量依赖性的抑制乳腺癌细胞系 BT-20，SUM149，MDA-MB-231，SK-BR-3，L226，SUM190，T147D，Cama-1 的增殖，ED50 为 1.3，1.5，8.1，1.6，2.0，2.0，2.5，2.5 μM，并诱导 Caspase-3 和 Caspase-7 的活性，不影响正常细胞的活力[2]。
TMI-1 (0-20 μM，48 h) 抑制乳腺癌细胞 SUM149 细胞周期，促进细胞凋亡并激活 Caspase-3，Caspase-7 ，Caspase-8，Caspase-9，增加了 ROS 的生成[2]。
TMI-1 (4 ng/mL，24 h) 改善紫杉醇 (HY-B0015) 诱导的 50B11 细胞的轴突的退行性变，并改善 forskolin (HY-15371) 诱导的神经突的生长，且具有剂量依赖性[3]。
TMI-1 (0.04-4 ng/mL，24 h) 剂量依赖性的减少 50B11 细胞的 TRPV1 蛋白表达，PKC，PI3K，NF-κB，TNF-α，IL-1β 和 IL-6 mRNA 的表达，减少钙内流[3]。

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

TMI-1 相关抗体:

Cell Cytotoxicity Assay[2]

Cell Line: SUM149, TgNeu 27
Concentration: 0, 5, 10, 15, 20 μM
Incubation Time: 5 days
Result: Inhibited breast cancer cell proliferation by dosage-dependent.

Cell Cycle Analysis[2]

Cell Line: SUM149
Concentration: 0, 2.5, 5, 10, 15, 20 μM
Incubation Time: 48 h
Result: Made G0/G1 phase cell cycle arrest.

Apoptosis Analysis[2]

Cell Line: SUM149, TgNeu 27
Concentration: 0, 1.25, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced cell apoptosis and activated Caspase-3, Caspase-7, Caspase-8, and Caspase-9 in a dose-dependent manner, while also increasing the generation of ROS.

Immunofluorescence[3]

Cell Line: 50B11 (induced by forskolin and paclitaxel)
Concentration: 4 ng/mL; 0.04, 0.4, 4 ng/mL
Incubation Time: 24 h
Result: Promoted the repair of axonal damage, improved the growth of neural projections, and had a dose-dependent effect.
Reduced intracellular calcium concentration.

Western Blot Analysis[3]

Cell Line: 50B11 (induced by forskolin and paclitaxel)
Concentration: 0.04, 0.4, 4 ng/mL
Incubation Time: 24 h
Result: Reduced the levels of the TRPV1 protein in a dose-dependent manner.

Real Time qPCR[3]

Cell Line: 50B11 (induced by forskolin and paclitaxel)
Concentration: 0.04, 0.4, 4 ng/mL
Incubation Time: 24 h
Result: Decreased the levels of PKC, PI3K, NF-κB, TNF-α、IL-1β and IL-6.
体内研究
(In Vivo)

TMI-1 (0-50 mg/kg，单次剂量，口服) 在 LPS 诱导的关节炎小鼠模型中抑制 TNF-α 分泌[1]。
TMI-1 (0-50 mg/kg，一天两次，14-17 天，口服) 在治疗性和预防性关节炎小鼠模型中均有效，降低了疾病严重程度[1]。
TMI-1 (100 mg/kg，每天一次，30 天，口服) 在乳腺癌小鼠模型中可减缓乳腺癌肿瘤生长，防止肿瘤发生[2]。
TMI-1 (100 mg/kg，每天一次，4 周，口服) 使促动脉粥样硬化的脂蛋白谱变化，但并未影响早期动脉粥样硬化病变的进展[4]。
Balb/CJ 小鼠单次口服 50 mg/kg 的药代动力学分析[1]

Route Dose (mg/kg) AUC (ng•h/mL) bioavailability (%) t1/2 (h) Cmax (μM)
oral 50 1484 39 1.68 3

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

Animal Model: LPS-induced acute arthritis mouse model [1]
Dosage: 0, 25, 50 mg/kg; single dose
Administration: Oral
Result: Inhibited the secretion of soluble TNF-α.
Animal Model: LPS or type II collagen-boost, and a therapeutic model with type II collagen-boost[1]
Dosage: 5, 10, 20 mg/kg; twice a day; 17 days
Administration: Oral
Result: Decreased in clinical severity scores in a dose-dependent.
Animal Model: Mouse model of arthritis induced by type II collagen[1]
Dosage: 100 mg/kg; twice a day; 14 days
Administration: Oral
Result: Decreased in clinical severity scores.
Animal Model: A faithful model of spontaneous mammary gland carcinogenesis due to overexpression of the ErbB2/neu proto-oncogene[2]
Dosage: 100 mg/kg; daily; 30 days
Administration: Oral
Result: Inhibited 82% of breast cancer tumor growth, and there were no new tumors appearing. The primary tumor shrank after treatment.
Animal Model: Male apolipoprotein E deficient (apoE-/-) mice[4]
Dosage: 100 mg/kg; daily; 4 weeks
Administration: Oral
Result: Caused a significant drop in soluble L-selectin levels in the plasma; in wild-type mice, inhibiting ADAM17 didn't significantly reduced L-selectin shedding, total cholesterol increased significantly by 28%, triglyceride levels rose by 113%, the levels of lipoproteins containing apolipoprotein B (very low-density lipoprotein VLDL and low-density lipoprotein LDL) went up, high-density lipoprotein HDL levels stayed the same, and there was no difference in the area of atherosclerotic lesions.
分子量

398.50

Formula

C17H22N2O5S2
CAS 号
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (250.94 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5094 mL 12.5471 mL 25.0941 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 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, 6 months; -20°C, 1 month。-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。

  • 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

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.59%

COA (289 KB) HNMR (164 KB) RP-HPLC (169 KB) MS (179 KB)

产品使用指南 (1538 KB)
参考文献

TMI-1 相关分类

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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5094 mL 12.5471 mL 25.0941 mL 62.7353 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 mL 12.5471 mL
10 mM 0.2509 mL 1.2547 mL 2.5094 mL 6.2735 mL
15 mM 0.1673 mL 0.8365 mL 1.6729 mL 4.1824 mL
20 mM 0.1255 mL 0.6274 mL 1.2547 mL 3.1368 mL
25 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5094 mL
30 mM 0.0836 mL 0.4182 mL 0.8365 mL 2.0912 mL
40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5684 mL
50 mM 0.0502 mL 0.2509 mL 0.5019 mL 1.2547 mL
60 mM 0.0418 mL 0.2091 mL 0.4182 mL 1.0456 mL
80 mM 0.0314 mL 0.1568 mL 0.3137 mL 0.7842 mL
100 mM 0.0251 mL 0.1255 mL 0.2509 mL 0.6274 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.

Keywords:

TMI-1287403-39-8WAY-171318TMI1TMI 1WAY171318WAY 171318MMPApoptosisInterleukin RelatedTNF ReceptorCaspaseMatrix metalloproteinasesILTumor Necrosis Factor ReceptorTNFRArthritisTumor growthInflammationNeurotoxicityArteriosclerosisInhibitorinhibitorinhibit

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