2. Apoptosis NF-κB MAPK/ERK Pathway
  3. TNF Receptor NF-κB Apoptosis p38 MAPK
  4. BMS-561392

BMS-561392 是一种选择性 ADAM17(TACE) 抑制剂。BMS-561392 可通过调控 p44 MAPK、NFκB 等信号通路抑制 TNF-α 分泌。BMS-561392 也会影响少突胶质细胞、小胶质细胞等中枢神经系统相关细胞的存活。BMS-561392 在小鼠脊髓损伤模型中可促进小胶质细胞凋亡 (apoptosis)，增大损伤范围并加重星形胶质细胞增生。BMS-561392 可用于脊髓损伤、炎症性疾病的相关研究。

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BMS-561392

BMS-561392 Chemical Structure

CAS No. : 611227-74-8

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BMS-561392 的其他形式现货产品:

Customer Review

Other Forms of BMS-561392:

BMS-561392 相关抗体

Top Publications Citing Use of Products

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-561392 is a selective ADAM17(TACE) inhibitor. BMS-561392 inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 can be used in research related to spinal cord injury and inflammatory diseases[1][2].

体外研究
(In Vitro)

BMS-561392 (10 nM；1-2.5 h) 可强效抑制重组人 TACE (ADAM17) 的酶活性，抑制率约为 80%[1]。
BMS-561392 (10 μM；5 h) 可有效抑制 RAW264.7 巨噬细胞中 LPS (HY-D1056) 诱导的 TNF-α 分泌[1]。
BMS-561392 (1-100 μM；5 h) 在 RAW264.7 巨噬细胞中呈剂量依赖性抑制 LPS 诱导的 p-IκB 表达，进而抑制 NF-κB 通路的激活[1]。
BMS-561392 (1-100 μM；2 h) 可抑制 RAW264.7 巨噬细胞中 LPS 诱导的 p-NFκB 表达，在 10 μM 和 100 μM 浓度下可轻度抑制 LPS 诱导的 p-ERK 表达[1]。
BMS-561392 (0.3-2.7 mM; 48 h) 可呈浓度依赖性降低未分化 HOG、MO3.13 细胞的活力，但对原代皮质神经元的活力无影响[2]。
BMS-561392 (0.3-2.7 mM；48 h) 以浓度依赖方式调控 BV-2 小胶质细胞的活力，孵育 48 h 后，0.3 mM 时细胞活力略有上升，1.3 mM 时下降 50%，2.7 mM 时下降 94%[2]。
BMS-561392 (1.3-2.7 mM) 可诱导 BV-2、MO3.13 细胞发生凋亡[2]。
BMS-561392 (0.3-2.7 mM; 3 h) 可提高 BV-2 小胶质细胞的膜 TNFR-1、TNFR-2 的表达，上调 pro-NGF 的表达[2]。
BMS-561392 (0.3-2.7 mM；3 h) 在 BV-2 小胶质细胞中以浓度依赖的方式调控磷酸化 p44 MAPK 的水平：孵育 3 h 后，0.3 mM 浓度下可升高该蛋白水平，2.7 mM 浓度下则使其检测不到，且对磷酸化 p42 MAPK 无影响[2]。

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

BMS-561392 相关抗体:

ELISA Assay[1]

Cell Line: RAW264.7 macrophage cells
Concentration: 10 μM (pre-incubation); 1 μg/mL (LPS stimulation)
Incubation Time: 1 h (pre-incubation); 4 h (LPS stimulation)
Result: Reduced LPS-induced TNF-α levels to near-control levels.

Western Blot Analysis[1]

Cell Line: RAW264.7 macrophage cells
Concentration: 1, 10 and 100 μM (pre-incubation); 1 μg/mL (LPS stimulation)
Incubation Time: 1 h (pre-incubation); 4 h (LPS stimulation)
Result: Induced a dose-dependent reduction in LPS-stimulated p-IκB levels.
体内研究
(In Vivo)

BMS-561392 (2.2 mM；皮下注射；每日给药；持续 15 天) 可显著抑制小鼠 SCI 损伤后运动功能的恢复，增大损伤面积并加重星形胶质细胞增生，减少小胶质细胞/巨噬细胞浸润，同时促进小胶质细胞凋亡[2]。

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

Animal Model: C57BL/6 (10-week-old)[2]
Dosage: 2.2 mM
Administration: s.c.; daily; 15 days
Result: Significantly reduced locomotor recovery as measured by BMS score.
Significantly increased lesion size.
Significantly increased astrogliosis in tissue caudal to the lesion site.
Significantly reduced Iba1 expression in tissue rostro-caudal to the lesion epicenter.
Significantly increased the number of apoptotic microglial/macrophage cells in tissue caudal to the lesion site.
Significantly increased pro-apoptotic Bax expression in spinal cord tissue.
Showed a non-significant decrease in anti-apoptotic Bcl-2 expression in spinal cord tissue.
分子量

476.57

Formula

C27H32N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BMS-561392 相关分类

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  • 稀释计算器

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  • 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:

BMS-561392611227-74-8DPC 333BMS561392BMS 561392DPC333DPC-333TNF ReceptorNF-κBApoptosisp38 MAPKTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBADAM17RAW264.7 macrophage cellsTNF-αmicrogliaBV-2 microglial cellscortical neuronsastrocytesoligodendrocytesp44 MAPKmouse spinal cord injury modelInhibitorinhibitorinhibit

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