2. Immunology/Inflammation Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Apoptosis
  3. COX VEGFR HIF/HIF Prolyl-Hydroxylase Caspase Bcl-2 Family Apoptosis MMP
  4. Multi-kinase-IN-8

Multi-kinase-IN-8 是一种多激酶抑制剂。Multi-kinase-IN-8 可抑制 COX-1 (IC50 = 12.6 μM), COX-2 (IC50 = 0.05 μM) 和 VEGFR-2 (IC50 = 0.12 nM)。Multi-kinase-IN-8 还能抑制肿瘤相关碳酸酐酶 CA IX 和 CA XII (其 Ki 分别为 31.5 和 386.9 nM)，并通过上调 Caspase-9 和 Bax 下调 Bcl-2 来触发细胞周期阻滞和细胞凋亡 (apoptosis) 。Multi-kinase-IN-8 可抑制 PGE2，p-VEGFR-2，MMP-9 及 HIF-1α 的表达，并对乳腺癌、肺癌和结直肠腺癌均表现出生长抑制活性。

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Multi-kinase-IN-8

Multi-kinase-IN-8 Chemical Structure

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Multi-kinase-IN-8 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

查看 VEGFR 亚型特异性产品:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

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HIF-1α HIF

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

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma[1].

IC50 & Target[1]

COX-2

0.05 μM (IC50)

COX-1

12.6 μM (IC50)

VEGFR2

0.12 nM (IC50)

体外研究
(In Vitro)

Multi-kinase-IN-8 (Compound 5j) 可抑制多种癌细胞系的增殖，其对 MDA-MB-231，MCF-7，A549 及 Caco-2 细胞的 IC50 值分别为 1.30 μM、 9.53 μM、 2.07 μM 和 2.28 μM[1]。
Multi-kinase-IN-8 (2.07 μM, 72 h) 在 Caco-2 中可抑制 VEGFR-2[1]。
Multi-kinase-IN-8 (24 h and 48 h) 可诱导 Caco-2 细胞周期阻滞于 G1 期[1]。
Multi-kinase-IN-8 (24 h and 48 h) 通过诱导在 Caco-2 细胞凋亡来引发细胞死亡[1]。
Multi-kinase-IN-8 (24 h and 48 h) 可下调 MDA-MB 231细胞中 HIF-1α mRNA 表达，并降低 PGE2 、总 VEGFR-2 及磷酸化VEGFR-2 的水平[1]。
Multi-kinase-IN-8 对肿瘤相关碳酸酐酶亚型（尤其是 hCA IX）具有选择性靶向潜力，这源于其与催化锌结合位点的相互作用[1]。
Multi-kinase-IN-8 在 Caco-2 细胞中可下调凋亡启动因子 Caspase-9 及线粒体凋亡标志物 Bcl-2 与 Bax 的表达水平[1]。

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

Multi-kinase-IN-8 相关抗体:

Cell Migration Assay [1]

Cell Line: Caco-2 cells
Concentration: 2.07 μM
Incubation Time: 72 h
Result: Suppressed Caco-2 cell migration with 56.29 % wound closure.

Cell Cycle Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased of % Caco-2 cells in G0 / G1 phase from 62.07 % in the control to 86.36 %.
Reduced nearly 3-fold in % Caco-2 cells in both S phase and G2 / M phase.

Apoptosis Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased 42 fold in total apoptosis.
Increased the ratio of annexin V-FITC positive early apoptotic cells from 0.54 % to 20.26 %, whilst the percentage of late apoptotic cells rose from 0.22 % to 11 %.
Resulted in a combined percentage of early and late apoptotic cells that significantly exceeded the percentage of necrotic cells. (Early apoptotic cells is 20.26%, late apoptotic cells is 11.32%, necrotic cells is 3.61%).
体内研究
(In Vivo)

Multi-kinase-IN-8 (Compound 5j) (50 mg/kg，皮下注射，5 天) 在雄性 BALB/c 小鼠体内建立的 MDA-MB-231移植瘤模型中显示出抗肿瘤活性[1]。

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

Animal Model: Cyclosporine (HY-100563A)-preconditioned (30 mg/kg/day, for 1 week) male BALB/c mice and then injected with MDA-MB 231 cells (1 × 106 per mouse)[1].
Dosage: 50 mg/kg
Administration: s.c., daily, five consecutive days, dissolved in 100 μL of DMSO (HY-Y0320C) /PBS (HY-K3005) (1:20, v/v).
Result: Reduced tumor size.
Induced 92.3 % tumor regression.
Had no significant changes in body weight were observed during the treatment course, indicating a satisfactory safety profile.
分子量

531.54

Formula

C25H21N7O5S
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

Multi-kinase-IN-8 相关分类

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  • 稀释计算器

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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:

Multi-kinase-IN-8COXVEGFRHIF/HIF Prolyl-HydroxylaseCaspaseBcl-2 FamilyApoptosisMMPCyclooxygenaseVascular endothelial growth factor receptorHypoxia-inducible factorsHIFsHIF-PHMatrix metalloproteinasesbreast cancerlung cancercolorectal adenocarcinomaInhibitorinhibitorinhibit

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