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

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.

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TKL002

TKL002 Chemical Structure

CAS No. : 3098518-95-4

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TKL002 Related Antibodies

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

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

 

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]
In Vitro

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.

TKL002 Related Antibodies

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.
In Vivo

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.
Molecular Weight

420.40

Formula

C21H20F4N4O
CAS No.
SMILES

COC1=CC=C(C2=C1)N=C(C=C2C(F)(F)F)NC3=CC=C(C(F)=C3)N4CCNCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TKL002 Related Classifications

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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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