2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin polymerization-IN-84

Tubulin polymerization-IN-84 通过靶向秋水仙碱结合口袋来抑制微管蛋白 (Tubulin) 聚合，IC50 为 10.9 μM。Tubulin polymerization-IN-84 对 Jurkat、B16-F10、HCT116 和 MDA-MB-231 细胞具有抗增殖活性 (IC50 分别为 60 nM、380 nM、138 nM 和 1.054 μM)。Tubulin polymerization-IN-84 可诱导 B16-F10 细胞发生 G2/M 期阻滞并诱导凋亡 (apoptosis)。Tubulin polymerization-IN-84在 B16-F10 黑色素瘤模型中抑制肿瘤生长，并在与 PD-L1 单抗联用时增强体内抗肿瘤免疫反应，适用于 T 细胞急性淋巴细胞白血病、黑色素瘤、结肠癌和乳腺癌的相关研究。

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Tubulin polymerization-IN-84

Tubulin polymerization-IN-84 Chemical Structure

CAS No. : 2982893-14-9

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Tubulin polymerization-IN-84 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.

体外研究
(In Vitro)

Tubulin polymerization-IN-84 (compound 5b) 可抑制 Jurkat、B16-F10、HCT116 和 MDA-MB-231 细胞增殖 (IC50 分别为 60 nM、380 nM、138 nM 和 1.054 μM)[1]。
Tubulin polymerization-IN-84 (0.1-5 μM; 24 h) 可剂量依赖性抑制 B16-F10 细胞的伤口愈合/迁移及克隆形成[1]。
Tubulin polymerization-IN-84 (0.5-5 μM；48 h) 可诱导 B16-F10 细胞 G2/M 期阻滞 (G2/M：对照 9.75%，5 μM 时 81.1%)[1]。
Tubulin polymerization-IN-84 (0.5-5 μM；48 h) 可诱导 B16-F10 细胞凋亡[1]。
Tubulin polymerization-IN-84 可与 β-tubulin 直接结合 (KD = 31.84 μM)[1]。
Tubulin polymerization-IN-84 (0.1-5 μM) 以浓度依赖的方式与 EBI 竞争结合 B16-F10 细胞中 β-微管蛋白的秋水仙碱结合位点[1]。
Tubulin polymerization-IN-84 (0.5-5 μM；12 h) 可导致 B16-F10 细胞胞质微管网络解聚[1]。
Tubulin polymerization-IN-84 (0.5-5 μM；6 h) 可剂量依赖性破坏 HUVEC 在 Matrigel 上的毛细血管样管网形成并减少连接点[1]。

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

Tubulin polymerization-IN-84 相关抗体:

Cell Migration Assay [1]

Cell Line: B16-F10
Concentration: 0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed wound closure and decreased migration rate versus control.

Cell Proliferation Assay[1]

Cell Line: B16-F10
Concentration: 0.5 μM; 1 μM; 5 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed colony formation and reduced colony numbers versus control.

Cell Cycle Analysis[1]

Cell Line: B16-F10
Concentration: 0.5 μM; 1 μM; 5 μM
Incubation Time: 48 h
Result: Increased the proportion of cells arrested at G2/M phase in a dose-dependent manner (9.75% in control vs 81.1% at 5 μM).

Apoptosis Analysis[1]

Cell Line: B16-F10
Concentration: 0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time: 48 h
Result: Increased total apoptotic cells in a dose-dependent manner (14.79% in control vs 21.22%/23.65%/35.66% at 0.5/1/5 μM).

Western Blot Analysis[1]

Cell Line: B16-F10
Concentration: 0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time: After treatment
Result: Competitively inhibited EBI-induced β-tubulin adduct formation in a concentration-dependent manner, indicating binding to the colchicine-binding site of β-tubulin.

Immunofluorescence[1]

Cell Line: B16-F10
Concentration: 0.5 μM; 1 μM; 5 μM
Incubation Time: 12 h
Result: Induced disassembly of cytoplasmic microtubule networks compared with control.
体内研究
(In Vivo)

Tubulin polymerization-IN-84 (compound 5b) (10 mg/kg；腹腔注射 i.p.；每日一次 QD；14 天) 可抑制 C57BL/6 小鼠 B16-F10 黑色素瘤肿瘤生长 (TGI = 27.5%) ，并在与 PD-L1 单抗联用 (10 + 10 mg/kg) 时进一步增强疗效 (TGI = 36.2%)，且未见显著体重下降[1]。

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

Animal Model: C57BL/6 mice bearing established B16-F10 melanoma tumors[1]
Dosage: 10 + 10 mg/kg (5b + PD-L1 mAb)
Administration: Intraperitoneal injection (i.p.); once daily (QD); for 14 days
Result: Inhibited tumor growth as monotherapy (TGI = 27.5%) and showed higher tumor growth inhibition in combination with PD-L1 mAb (TGI = 36.2%), without significant body-weight loss.
Increased the proportion of activated CD3+CD8+ cytotoxic T cells in tumors (48.9% in combination group vs 31.8% in control).
Reduced Ki-67 expression and increased γ-H2AX signals in tumor tissues.
Showed no apparent histopathological abnormalities in major organs and no significant changes in serum biochemistry markers versus control.
分子量

374.43

Formula

C23H22N2O3
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

Tubulin polymerization-IN-84 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin polymerization-IN-842982893-14-9Microtubule/TubulinApoptosistubulin polymerization inhibitorcolchicine-binding sitemicrotubule destabilizermelanomaPD-L1 mAbimmune potentiationB16-F10Inhibitorinhibitorinhibit

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