2. Cytoskeleton Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Myosin Ferlin Family MMP
  4. Myoferlin inhibitor 1

Myoferlin inhibitor 1 与肌成纤维蛋白 (myoferlin) MYOF-C2D 表现出可逆的、浓度依赖性的结合，其 KD值 为 0.094 μM。Myoferlin inhibitor 1 对不同胰腺癌细胞表现出强大的抗侵袭和抗迁移活性。Myoferlin inhibitor 1 通过逆转间充质转化 (EMT) 、抑制 MMP1 和 MMP2 的分泌以及阻断受体酪氨酸激酶来抑制胰腺癌转移。Myoferlin inhibitor 1 在体外和体内均表现出对胰腺癌有效的抗转移活性。Myoferlin inhibitor 1 可用于预防胰腺癌转移的研究。

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Myoferlin inhibitor 1

Myoferlin inhibitor 1 Chemical Structure

CAS No. : 2366279-99-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥940
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5 mg ￥855
In-stock
10 mg ￥1350
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25 mg ￥2700
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50 mg ￥4320
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Myoferlin inhibitor 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Myoferlin inhibitor 1 is a compound that exhibits reversible, concentration-dependent binding to the myoferlin MYOF-C2D protein, with a KD of 0.094 μM. Myoferlin inhibitor 1 shows potent anti-invasion and anti-migration activities against different pancreatic cancer cells. Myoferlin inhibitor 1 inhibits pancreatic cancer metastasis through reversing mesenchymal transition (EMT), inhibiting the secretions of MMP1 and MMP2 and blocking the receptor tyrosine kinases. Myoferlin inhibitor 1 displays effective antimetastatic activities in pancreatic cancer in vitro and in vivo. Myoferlin inhibitor 1 can be used in research on preventing pancreatic cancer metastasis[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Capan-2 IC50
2.85 μM
Compound: 6y
Cytotoxicity against human Capan2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Cytotoxicity against human Capan2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
[PMID: 31026162]
MCF-10A IC50
27.56 μM
Compound: 6y
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
[PMID: 31026162]
MIA PaCa-2 IC50
1.54 μM
Compound: 6y
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
[PMID: 31026162]
PANC-1 IC50
0.11 μM
Compound: 6y
Antimigratory activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based transwell assay
Antimigratory activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based transwell assay
[PMID: 31026162]
PANC-1 IC50
0.12 μM
Compound: 6y
Antiinvasive activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based matrigel coated transwell assay
Antiinvasive activity against human PANC1 cells measured after 18 hrs in presence of mitomycin C using crystal violet staining by inverted microscopy-based matrigel coated transwell assay
[PMID: 31026162]
PANC-1 IC50
0.84 μM
Compound: 6y
Cytotoxicity against human PANC1 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
Cytotoxicity against human PANC1 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
[PMID: 31026162]
体外研究
(In Vitro)

Myoferlin inhibitor 1 (compound 6y) (18 小时) 抑制 PANC1 细胞的侵袭，IC50 为 0.12 μM[1]。
Myoferlin inhibitor 1 (100-400 nM，18-36 小时) 以浓度依赖性方式抑制 PANC1、 MiaPaCa2 和 Capan2 细胞的迁移[1]。
Myoferlin inhibitor 1 (48 小时) 在三种胰腺癌细胞系 (PANC-1、 MIA PaCa-2 和 Capan-2) 中表现出细胞毒性，IC50 值分别为 0.84、1.54 和 2.85 μM，在三种人类正常细胞系 (HAF、 HPDE6-C7 和 MCF-10A) 中表现出细胞毒性，IC50 值分别为 8.54、14.64 和 27.56 μM [1]。
Myoferlin inhibitor 1 (0-400 nM，18 小时) 表现出抗迁移作用，并与 PANC1 细胞中的 MYOF 表达呈正相关[1]。
Myoferlin inhibitor 1 (0-400 nM，0-24 小时) 可使胰腺癌细胞逆转至上皮状态，抑制 MMP1 和 MMP2 的分泌，并通过 VEGF 和 EGFR 信号通路以剂量依赖性方式抑制肿瘤转移[1]。
Myoferlin inhibitor 1 (0.05-50 μM) 对受试的人类 CYP 酶表现出较弱的抑制作用，尤其对 CYP2C9 的活性较低[1]。

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

Myoferlin inhibitor 1 相关抗体:

Cell Migration Assay [1]

Cell Line: PANC1, MiaPaCa2, and Capan2 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 18 h for PANC1, 24 h for MiaPaCa2, and 36 h for Capan2
Result: Reduced migrated cell numbers of PANC1, MiaPaCa2 and Capan2 cells in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: PANC1 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 15, 30, 60, 120 min and 24 h
Result: Increased the expression of the epithelial marker E-cadherin and decreased that of the mesenchymal marker fibronectin in a concentration-dependent manner.
Decreased the levels of MMP1 and MMP2 in PANC1 cells in a concentration-dependent manner.
Depressed the phosphorylation of VEGFR induced by VEGF.
Caused sustained EGFR phosphorylation upon 10 ng/mL EGF stimulation, thereby preventing the deactivation of the EGFR signaling pathway.
体内研究
(In Vivo)

Myoferlin inhibitor 1 (25 和 50 mg/kg，腹腔注射，每日一次，共 21 天) 具有强大的抗转移活性，可在胰腺癌肺转移小鼠模型中提高总体生存率，且无明显毒性[1]。

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

Animal Model: BALB/c nude mice (8 weeks old) intravenously injected with PANC1-luc cancer cells[1]
Dosage: 25 and 50 mg/kg
Administration: i.p., daily for 21 days
Result: Dose-dependently inhibited pancreatic cancer pulmonary metastasis with superior antitumor metastatic activity compared to the positive control at the same dosage.
Significantly prolonged the overall survival, resulting in survival rates of 75 % at 25 mg/kg and 87.5 % at 50 mg/kg.
Revealed no significant toxicity in the major organs (heart, lung, liver, spleen, and kidney).
分子量

456.54

Formula

C26H28N6O2
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
4°C 2 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 : 50 mg/mL (109.52 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 2.1904 mL 10.9519 mL 21.9039 mL
5 mM 0.4381 mL 2.1904 mL 4.3808 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
参考文献

Myoferlin inhibitor 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 2.1904 mL 10.9519 mL 21.9039 mL 54.7597 mL
5 mM 0.4381 mL 2.1904 mL 4.3808 mL 10.9519 mL
10 mM 0.2190 mL 1.0952 mL 2.1904 mL 5.4760 mL
15 mM 0.1460 mL 0.7301 mL 1.4603 mL 3.6506 mL
20 mM 0.1095 mL 0.5476 mL 1.0952 mL 2.7380 mL
25 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
30 mM 0.0730 mL 0.3651 mL 0.7301 mL 1.8253 mL
40 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3690 mL
50 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
60 mM 0.0365 mL 0.1825 mL 0.3651 mL 0.9127 mL
80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
100 mM 0.0219 mL 0.1095 mL 0.2190 mL 0.5476 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:

Myoferlin inhibitor 12366279-99-2Myoferlin inhibitor1Myoferlin inhibitor-1MyosinFerlin FamilyMMPMatrix metalloproteinasespancreatic cancerPANC1MiaPaCa2Capan2MMP1MMP2receptor tyrosine kinasesanti-invasionanti-migrationantimetastaticmetastasisPANC1-luc cancer cellspancreatic cancer lung metastasis mice modelInhibitorinhibitorinhibit

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