2. PI3K/Akt/mTOR MAPK/ERK Pathway NF-κB
  3. PI3K Akt mTOR p38 MAPK NF-κB
  4. Calebin A

Calebin A 是一种具有口服活性的 PI3K/Akt/mTOR、MAPK 和 NF-κB 抑制剂。Calebin A 可阻断自噬抑制作用，抑制细胞凋亡。Calebin A 可通过表观遗传调控发挥抗肿瘤活性。Calebin A 可抑制脂肪生成、调节产热并富集肠道益生菌。Calebin A 可用于骨关节炎、阿尔茨海默病、2 型糖尿病、恶性外周神经鞘瘤及结直肠癌的相关研究。

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Calebin A

Calebin A Chemical Structure

CAS No. : 336784-82-8

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Calebin A 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

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer[1][2][3][4][5].

体外研究
(In Vitro)

Calebin A (5 μM) 可在骨关节炎环境培养的原代犬软骨细胞中抑制细胞凋亡并促进自噬相关蛋白 Beclin-1 的表达[1]。
Calebin A (5 μM) 可在骨关节炎环境中培养的原代犬软骨细胞中上调 ECM 和自噬标志物，下调炎症、降解、凋亡以及mTOR/PI3K/Akt 信号通路，其作用依赖于完整的自噬过程[1]。
Calebin A 可通过调控 TNF-β/NF-κB 信号通路及相关生物标志物，抑制 HCT116、RKO 和 SW480 结直肠癌细胞的结肠癌球形成、增殖、侵袭/迁移能力，并促进其细胞凋亡[2]。
Calebin A 可逆转长春新碱耐药性，通过调控 MAPK 信号通路和 P-糖蛋白在 SGC7901 胃癌细胞中诱导 G2/M 期阻滞与细胞凋亡[2]。
Calebin A 可抑制 Sup-T1 淋巴瘤细胞的生长并降低其活力，还可调控表观遗传酶 (HAT, HDAC, PCAF)[2]。
Calebin A 可通过 NF-κB/Scleraxis 信号通路下调犬肌腱细胞的炎症反应[2]。
Calebin A (20 μM) 可抑制脂肪细胞的脂肪生成并诱导其脂解，且 20 μM 浓度下即可诱导脂解[2]。
Calebin A (25 μM；24 h) 可诱导 STS26T、S462-TY、ST8814 和 T265 型 MPNST 细胞的 G2/M 期占比降低、G1 期占比升高，从而阻滞细胞周期进程[3]。
Calebin A (12.5-25 μM) 可下调 MPNST 细胞中磷酸化 AKT、磷酸化 ERK1/2、survivin、hTERT 及乙酰化组蛋白 H3 的表达[3]。

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

Calebin A 相关抗体:

Cell Proliferation Assay[3]

Cell Line: S462-TY, ST8814, T265, STS26T MPNST cell lines; LinNF primary neurofibroma cells
Concentration: 6.25, 12.5, 25, 50, 100 μM
Incubation Time: 24 h
Result: Decreased viability of MPNST cell lines at 12.5-25 μM; reduced survival by less than 50% in all MPNST cell lines with 25 μM treatment; inhibited growth of primary neurofibroma cells.

Cell Cycle Analysis[3]

Cell Line: STS26T, S462-TY, ST8814, T265 MPNST cell lines
Concentration: 25 μM
Incubation Time: 24 h
Result: Decreased STS26T cells in G2/M phase from 12.6% to 11.4% and increased G1 phase from 73.6% to 74.6%; reduced S462-TY G2/M phase from 19.7% to 8.8%, ST8814 G2/M phase from 6.4% to 6.0%, and T265 G2/M phase from 23.1% to 18.3%.

Cell Proliferation Assay[5]

Cell Line: HCT116 colorectal cancer cells (co-cultured with MRC-5 fibroblasts and Jurkat T-lymphocytes in multicellular proinflammatory TME; or co-cultured with MRC-5 fibroblasts and 10 ng/ml TNF-β in TNF-β-TME)
Concentration: 1-5 μM (10 days treatments); 5 μM (4 h immunofluorescence assay)
Incubation Time: 10 days (MTT, colonosphere, invasion, Western blotting); 4 h (immunofluorescence)
Result: Dose-dependently inhibited HCT116 cell proliferation, with maximum inhibition at 5 μM. Reduced colonosphere formation and invasion dose-dependently. Decreased nuclear p65-NF-κB labeling to 21% in multicellular TME and 22% in TNF-β-TME at 5 μM after 4 h treatment. Increased apoptosis to 59% in multicellular TME and 48% in TNF-β-TME at 5 μM after 4 h treatment. Suppressed p65-NF-κB phosphorylation, NF-κB-regulated gene products (MMP-9, CXCR4, Ki-67, β1-integrin), and cancer stem cell markers (CD133, CD44, ALDH1) dose-dependently. Increased cleaved caspase-3 dose-dependently.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat 20 mg/kg i.v. T1/2 3.43 μg/mL
Rat 20 mg/kg i.v. CLtotal 61 L/h/kg
Rat 20 mg/kg i.v. CLrenal 0.11 L/h/kg
Rat 20 mg/kg i.v. CLhepatic 60.9 L/h/kg
Rat 100 mg/kg p.o. T1/2 1.18 μg/mL
Rat 100 mg/kg p.o. CLtotal 11244.3 L/h/kg
Rat 100 mg/kg p.o. CLrenal 0.274 L/h/kg
Rat 100 mg/kg p.o. CLhepatic 11244.0 L/h/kg
体内研究
(In Vivo)

Calebin A (100 mg/kg/d; p.o.; daily; 90 days) 经口给予雌雄 Wistar 大鼠 90 天具有安全性，未观察到毒性反应[2]。
Calebin A (500 mg/kg；灌胃；单次给药) 在雄性 Sprague-Dawley 大鼠中表现出如下药代动力学特征：生物利用度约为 0.5%，血清半衰期为 1-3 小时，且主要通过非肾脏途径排泄[2]。
Calebin A (100 mg/kg；腹腔注射；每周 3 次；持续 15 天) 在小鼠 MPNST 模型中可显著降低异种移植瘤的体积[3]。
Calebin A (0.1-0.5%；膳食补充；每日；12 周) 在高脂饮食诱导的肥胖小鼠中展现出剂量依赖性的抗肥胖作用，具体机制包括降低体重与血糖、恢复肝脏重量、增强适应性产热以及调节肠道菌群组成[4]。

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

Animal Model: Balb/c nude (male, 4 weeks old, MPNST xenograft model with S462-TY cells)[3]
Dosage: 100 mg/kg
Administration: i.p.; three times a week; 15 days
Result: Significantly decreased xenograft tumor size two weeks post-treatment.
Animal Model: C57BL/6 (male, 4 weeks old, high-fat diet-induced obesity)[4]
Dosage: 0.1%; 0.5%
Administration: high-fat diet (HFD) supplementation; daily; 12 weeks
Result: Reduced body weight in a dose-dependent manner; lowered fasting blood glucose and liver weight to normal diet levels (0.5% dose); decreased weights of white, beige, and brown adipose tissues (0.5% dose); improved liver color by reducing lipid accumulation (0.5% dose); better maintained rectal temperature with a higher area under the curve for temperature change than the high-fat diet group during 4°C cold exposure (0.5% dose); reduced Firmicutes-to-Bacteroidetes ratio from 1.24 ± 0.29 to 1.03 ± 0.42 (0.5% dose); increased Verrucomicrobia phylum abundance from 0.002 ± 0.001 to 0.022 ± 0.02 (0.5% dose); enriched genera including Akkermansia, Butyricicoccus, Ruminiclostridium_9, and unidentified_Ruminococcaceae (0.5% dose).
分子量

384.38

Formula

C21H20O7
CAS 号
结构分类
初始来源
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

Calebin A 相关分类

  • 摩尔计算器

  • 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:

Calebin A336784-82-8PI3KAktmTORp38 MAPKNF-κBPhosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinNuclear factor-κBNuclear factor-kappaBextracellular signal-regulated kinase (ERK)histone acetyltransferase (HAT)c-Jun N-terminal kinase (JNK)cyclooxygenase-2 (COX-2)MMP9Wistar ratsInhibitorinhibitorinhibit

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