2. NF-κB Apoptosis Cytoskeleton
  3. NF-κB Apoptosis Cadherin Caspase Bcl-2 Family
  4. TKL002

TKL002 是一种可穿透血脑屏障的 CTH/H2S/NF-κB/EMT 信号轴抑制剂。TKL002 可诱导胶质母细胞瘤细胞发生 G2/M 期细胞周期阻滞和细胞凋亡 (apoptosis)。TKL002 可通过上调 E-钙粘蛋白、下调 N-钙粘蛋白和波形蛋白来抑制胶质母细胞瘤细胞的迁移和侵袭。TKL002 可用于胶质母细胞瘤的相关研究。

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TKL002

TKL002 Chemical Structure

CAS No. : 3098518-95-4

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TKL002 相关抗体

Top Publications Citing Use of Products

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 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H2S/NF-κB/EMT signaling axis. TKL002 induces G2/M phase cell cycle arrest and apoptosis in glioblastoma cells. TKL002 inhibits the migration and invasion of glioblastoma cells by upregulating E-cadherin and downregulating N-cadherin and vimentin. TKL002 is applicable to relevant research on glioblastoma[1].

IC50 & Target[1]

NF-κB

 

Caspase 3

 

Bax

 

Bcl-2

 

体外研究
(In Vitro)

TKL002 (0.625-10 μM; 24-72 h) 可呈剂量和时间依赖性强效抑制 U87MG、U118MG 和 U251MG 胶质母细胞瘤细胞的增殖，且对正常 LX2 细胞具有选择性，在各细胞系和时间点的 IC50 值范围为 4.141 至 6.506 μM[1]。
TKL002 (6 μM; 48 h) 可诱导 U87MG 胶质母细胞瘤细胞发生晚期凋亡，该过程由 Bax 和 caspase-3 的上调以及 Bcl-2 和 active-caspase-3 的下调介导[1]。
TKL002 (2-6 μM; 24 h) 以浓度依赖的方式诱导 U87MG 和 U118MG 胶质母细胞瘤细胞发生 G2/M 期细胞周期阻滞[1]。
TKL002 (2-6 μM; 48 h) 可降低 U87MG 和 U118MG 胶质母细胞瘤细胞中 CTH、半胱氨酸及 H2S 的水平，提升 GSH 水平，并以剂量依赖的方式抑制 NF-κB 信号通路及促炎细胞因子的表达[1]。
TKL002 (2-6 μM ; 48 h) 以剂量依赖方式抑制 U87MG 和 U118MG 胶质母细胞瘤细胞的迁移与侵袭，该作用通过上调 E-cadherin、下调 N-cadherin 和 vimentin 来抑制上皮-间质转化[1]。

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

TKL002 相关抗体:

Apoptosis Analysis[1]

Cell Line: U87MG
Concentration: 2, 4, 6 μM
Incubation Time: 48 h
Result: Increased late apoptosis to 22.63%.

Cell Cycle Analysis[1]

Cell Line: U87MG, U118MG glioblastoma cells
Concentration: 2, 4, 6 μM
Incubation Time: 24 h
Result: Increased the G2/M phase fraction in a concentration-dependent manner.

Cell Migration Assay [1]

Cell Line: U87MG, U118MG glioblastoma cells
Concentration: 2, 4, 6 μM
Incubation Time: 48 h
Result: Inhibited GBM cell migration.

Cell Invasion Assay[1]

Cell Line: U87MG, U118MG glioblastoma cells
Concentration: 2, 4, 6 μM
Incubation Time: 48 h
Result: Inhibited GBM cell invasion.
体内研究
(In Vivo)

TKL002 (5-20 mg/kg; i.p.; 每隔一天一次，共 7 次) 以剂量依赖方式抑制胶质母细胞瘤皮下移植瘤的生长[1]。
TKL002 (10-20 mg/kg; i.v. 每三天一次共 5 次) 可穿过血脑屏障，以剂量依赖的方式抑制原位胶质母细胞瘤的生长，减少肿瘤负荷并维持小鼠身体状态，且无明显的器官毒性[1]。

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

Animal Model: BALB/c nude (male, 4−5 weeks old, 16−18 g, subcutaneous xenograft model)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.p.; every other day; 7 total doses
Result: Reduced mean subcutaneous tumor weight to 1.117 g (5 mg/kg) and 0.530 g, compared to 1.458 g in vehicle control.
Achieved similar tumor weight and volume reduction as 5 mg/kg temozolomide at 20 mg/kg.
Showed dose-dependent reductions in splenic index.
Caused minimal pathological changes in liver, spleen, and kidney; no significant changes in heart, liver, lung, or kidney indices.
Animal Model: BALB/c nude (male, 4−5 weeks old, 16−18 g, orthotopic xenograft model)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v. via tail vein; every 3 days; 5 total doses
Result: Reduced in vivo bioluminescent signal intensity to 13.62×104 photons/s (10 mg/kg) and 8.52×104 photons/s (20 mg/kg) on days 15 and 20, versus 25.21×104 photons/s in vehicle control.
Reduced ex vivo tumor bioluminescent signal intensity to 21.48×104 photons/s (10 mg/kg) and 9.20×104 photons/s (20 mg/kg), versus 63.88×104 photons/s in controls.
Maintained normal body condition in 20 mg/kg group, while control mice exhibited weight loss, reduced activity, and cachexia.
Showed marked, dose-dependent reductions in CTH-positive tumor area, with the 20 mg/kg group showing the most pronounced decrease.
Showed a higher survival rate in the 20 mg/kg group, though the difference was not statistically significant.
Caused no significant differences in organ indices among groups.
分子量

420.40

Formula

C21H20F4N4O
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

TKL002 相关分类

  • 摩尔计算器

  • 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:

TKL0023098518-95-4TKL 002TKL-002NF-κBApoptosisCadherinCaspaseBcl-2 FamilyNuclear factor-κBNuclear factor-kappaBU118MGCystathionine γ-lyase (CTH)U251MGglioblastomapro-inflammatory cytokineU87MGG2/M cell cycle arresthydrogen sulfideapoptosisInhibitorinhibitorinhibit

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