製品番号: HY-181717

TKL002

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Based on 1 Customer Validation

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.08%
CAS 番号: 3098518-95-4
分子式: C₂₁H₂₀F₄N₄O
分子量:420.40

保管条件:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

TKL002 構造式

CAS 番号: 3098518-95-4

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

NF-κB

Caspase 3

Bax

Bcl-2

NF-κB アイソフォーム固有の製品をすべて表示 :

Caspase アイソフォーム固有の製品をすべて表示 :

Bcl-2 Family アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	1.62 μM Compound: 7d	Cytotoxicity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay	[PMID: 39908792]

体外実験

TKL002 (0.625-10 μmol/L; 24-72 h) potently inhibits the proliferation of U87MG, U118MG, and U251MG glioblastoma cells in a dose- and time-dependent manner with selectivity over normal LX2 cells, exhibiting IC₅₀ values ranging from 4.141 to 6.506 μmol/L across cell lines and time points^[1].
TKL002 (6 μmol/L; 48 h) induces late apoptosis in U87MG glioblastoma cells, mediated via upregulation of Bax and caspase-3 and downregulation of Bcl-2 and active-caspase-3^[1].
TKL002 (2-6 μmol/L; 24 h) induces G₂/M phase cell cycle arrest in U87MG and U118MG glioblastoma cells in a concentration-dependent manner, with maximum G₂/M fractions of 22.68% and 30.31% at 6 μmol/L respectively^[1].
TKL002 (2-6 μmol/L; 48 h) reduces CTH, cysteine, and H₂S levels, increases GSH levels, and inhibits NF-κB signaling and pro-inflammatory cytokine expression in U87MG and U118MG glioblastoma cells in vitro in a dose-dependent manner^[1].
TKL002 (2-6 μmol/L; 48 h) inhibits migration and invasion of U87MG and U118MG glioblastoma cells in a dose-dependent manner, mediated via upregulation of E-cadherin and downregulation of N-cadherin and vimentin to suppress epithelial-mesenchymal transition^[1].

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

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.

体内実験

TKL002 (5-20 mg/kg; i.p.; once every other day, 7 total administrations) inhibits the growth of subcutaneous glioblastoma xenografts in a dose-dependent manner^[1].
TKL002 (10-20 mg/kg; i.v., once every three days for a total of 5 administrations) can cross the blood-brain barrier, inhibit the growth of orthotopic glioblastoma in a dose-dependent manner, reduce tumor burden, maintain the physical condition of mice, and cause no obvious organ toxicity^[1].

MedChemExpress (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.

化学情報

CAS 番号 3098518-95-4
性状 Solid
分子量 420.40
分子式 C₂₁H₂₀F₄N₄O
Color Light yellow to yellow
SMILES

COC1=CC=C(C2=C1)N=C(C=C2C(F)(F)F)NC3=CC=C(C(F)=C3)N4CCNCC4
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Luo Z, et al. Hijacking the Hydrogen Sulfide Axis: A Novel 4-Trifluoromethylquinoline Derivative Suppresses Glioblastoma via Cystathionine γ-Lyase Suppression. J Med Chem. 2026;69(3):3457-3476. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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TKL002

Apoptosis Compound Library

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

NF-κB アイソフォーム固有の製品をすべて表示

Caspase アイソフォーム固有の製品をすべて表示

Bcl-2 Family アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

TKL002 関連分類

HY-181717 関連分類