2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling MAPK/ERK Pathway Apoptosis Cell Cycle/DNA Damage
  3. Glycosidase NF-κB COX STAT ERK p38 MAPK Apoptosis CDK Survivin Bcl-2 Family
  4. G721-0282

G721-0282 是一种口服有效的 CHI3L1 抑制剂。G721-0282 可以降低炎性蛋白和细胞因子的表达。G721-0282 抑制 NF-κB 信号通路的激活。G721-0282 抑制神经炎症并减少焦虑行为。G721-0282 通过抑制 STAT3 信号通路显著抑制骨肉瘤 (OS) 细胞的增殖。G721-0282 通过上调促凋亡蛋白水平和下调抗凋亡蛋白水平诱导 OS 细胞凋亡 (apoptosis)。G721-0282 可用于神经炎症性疾病和癌症的研究。

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G721-0282 Chemical Structure

G721-0282 Chemical Structure

CAS No. : 946378-12-7

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G721-0282 相关抗体

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

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STAT3 STAT5 STAT6 STAT1

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of Osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro apoptotic protein levels and downregulating anti apoptotic protein levels. G721-0282 can be used for research on neuroinflammatory conditions and cancer[1][2].

IC50 & Target

CDK4

 

CDK6

 

COX-2

 

Bcl-2

 

p38

 

ERK

 

p-STAT3

 

NF-κB

 

体外研究
(In Vitro)

G721-0282 (5-20 μM) 可以抑制 BV-2 细胞内 LPS (HY-D1056) 诱导的神经炎症，包括 NO 的产生，促炎细胞因子的表达和炎症蛋白的水平[1]。
G721-0282 (20 μM) 在 BV-2 细胞内依赖于 CHI3L1 发挥抗炎作用[1]。
G721-0282 (10-50 μM，24-72小时) 以剂量依赖和时间依赖的方式抑制 MG63 和 U2OS 细胞的增殖[2]。
G721-0282 (0-50 μM, 24 小时) 可以通过下调抗凋亡蛋白水平和上调促凋亡蛋白水平来阻断 MG63 和 U2OS 细胞的细胞周期并诱导细胞凋亡[2]。
G721-0282 (0-50 μM, 12-48 小时) 通过抑制 STAT3 信号通路显著抑制 MG63 和 U2OS 细胞的迁移和侵袭能力[2]。
G721-0282 (2-4 周) 抑制骨肉瘤 (OS) 细胞在软琼脂中的集落形成能力[2]。
G721-0282 (0-50 μM，24 小时) 可降低 MMP2 和 MMP9 的水平[2]。

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

G721-0282 相关抗体:

Western Blot Analysis[2]

Cell Line: MG63 and U2OS cells
Concentration: 10, 30 and 50 μM
Incubation Time: 24 h
Result: Significantly reduced the level of Cyclin D1, cdk4, cdk6, ERK1/2, JNK, p38, Src, STAT3, Survivin, and Bcl-2 and increased the level of cleaved PARP and Cleaved caspase-3.
体内研究
(In Vivo)

G721-0282 (2.5 和 5 mg/kg; 口服; 每周两次; 持续 4 周) 显著减少了雄性 BALB/c 小鼠体内慢性不可预测的轻度应激 (CUMS) 引起的焦虑样行为，并抑制了神经炎症[1]。
G721-0282 (18.9 mg/kg; 腹腔注射; 每周两次; 持续 35 天) 在携带 MG63 肿瘤的雄性 BALB/c 无胸腺裸鼠中具有显著的抗肿瘤活性[2]。

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

Animal Model: CUMS-induced male BALB/c mice (8 weeks)[1]
Dosage: 2.5 and 5 mg/kg
Administration: Oral administration (p.o.); twice a week for 4 weeks
Result: Significantly reduced anxiety behavior in mice.
Significantly reduced the expression of inflammatory proteins, including iNOS, COX-2, IBA-1, p65, p50 and p-IκBα.
Reduced the expression of inflammatory factors, including TNF-α, IL-1β, and IL-6.
Inhibited the NF-κB signaling pathway.
Decreased the expression of CHI3L1 and IGFBP3 induced by CUMS.
Animal Model: 1×108 MG63 cells injected male BALB/c athymic nude mice (6 weeks)[2]
Dosage: 18.9 mg/kg
Administration: Intraperitoneal injection (i.p.); two times a week for 35 days
Result: Significantly inhibited tumor volume and weight.
Reduced the expression of CHI3L1, PCNA, Cyclin D1, and p-STAT3 in tumor tissue.
分子量

376.47

Formula

C18H24N4O3S
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

G721-0282 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:

G721-0282946378-12-7GlycosidaseNF-κBCOXSTATERKp38 MAPKApoptosisCDKSurvivinBcl-2 FamilyNuclear factor-κBNuclear factor-kappaBCyclooxygenaseExtracellular signal regulated kinasesCyclin dependent kinaseCHI3L1neuroinflammationanxietyCUMScancerapoptosisSTAT3MAPKInhibitorinhibitorinhibit

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