2. Apoptosis
  3. Apoptosis
  4. TMLZ-G46

TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research.

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TMLZ-G46

TMLZ-G46 Chemical Structure

CAS No. : 3116767-83-7

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TMLZ-G46 Related Antibodies

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Description

TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research[1].

In Vitro

TMLZ-G46 (10 μM; 3 h) binds to ZNF207 in LN229 and U251MG glioma cells, and significantly increases the thermal stability of this protein[1].
TMLZ-G46 (72 h) potently inhibits the proliferation of glioma cell lines with high ZNF207 expression (LN229, U251MG, HS683, T98G), with IC50 values below 3 μM, while its activity decreases in cell lines with low ZNF207 expression (U87MG, U118MG, U138MG)[1].
TMLZ-G46 (0.25-4 μM; 14 days) potently impairs the clonogenic capacity of LN229 and U251MG glioma cells, with significant inhibitory effects observable at concentrations as low as 0.25 μM[1].
TMLZ-G46 (10 days) selectively inhibits the self-renewal of glioma stem-like cells in LN229 and U251MG cells, with an IC50 value at the submicromolar level[1].
TMLZ-G46 (0.5-4 μM; 24 h) dose-dependently inhibits the expression of SOX2 in LN229 and U251MG glioma cells, providing a basis for its inhibition of stem cell properties[1].
TMLZ-G46 (0-8 μM; 24-48 h) inhibits the migration and invasion abilities of LN229 and U251MG glioma cells in a dose-dependent manner[1].
TMLZ-G46 (1-5 μM; 24 h) induces G0/G1 cell cycle arrest and apoptosis in LN229 and U251MG glioma cells[1].

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

TMLZ-G46 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: LN229 glioma cell line, U251MG glioma cell line, HS683 glioma cell line, U87MG glioma cell line, U118MG glioma cell line, U138MG glioma cell line, T98G glioma cell line
Concentration: /
Incubation Time: 72 h
Result: Showed potent antiproliferative activity, with half-maximal inhibitory concentration (IC50) values of 0.93 μM (LN229), 1.33 μM (U251MG), 2.07 μM (HS683), 2.05 μM (T98G), 4.82 μM (U87MG), 5.58 μM (U118MG), and 7.73 μM (U138MG).

Western Blot Analysis[1]

Cell Line: LN229 glioma cell line, U251MG glioma cell line
Concentration: 0.5, 1, 2, 4 μM
Incubation Time: 24 h
Result: Downregulated SOX2 protein expression in a dose-dependent manner in both cell lines, with significant reduction observed at 2 μM and 4 μM.

Cell Cycle Analysis[1]

Cell Line: LN229 glioma cell line, U251MG glioma cell line
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Induced G0/G1 cell cycle arrest.
Increased the G0/G1 fraction from 37.2% to 48.7% in LN229 cells at 5 μM.
Increased the G0/G1 fraction from 44.8% to 51.4% in U251MG cells at 5 μM.

Apoptosis Analysis[1]

Cell Line: LN229 glioma cell line, U251MG glioma cell line
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Induced apoptosis.
Reached apoptotic rates of 52.3% in LN229 cells at 5 μM.
Reached apoptotic rates of 12.5% in U251MG cells at 5 μM.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT F CL
Rat[1] 5 (male) mg/kg i.v. 0.31 h 0.083 h 2290.90 ng/mL 2546.66 ng·h/mL 0.44 h / 76.67 mL/min
Rat[1] 30 (male) mg/kg p.o. 11.90 h 5.17 h 592.79 ng/mL 10405.67 ng·h/mL 19.52 h 68.1 % /
Rat[1] 5 (female) mg/kg i.v. 0.28 h 0.083 h 1772.01 ng/mL 2006.24 ng·h/mL 0.41 h / 130 mL/min
Rat[1] 30 (female) mg/kg p.o. 14.7 h 3.24 h 327.53 ng/mL 6340.88 ng·h/mL 22.24 h 52.7 % /
In Vivo

TMLZ-G46 (60 mg/kg; p.o.; once daily; 28 days) achieves a tumor growth inhibition rate of 83.7% in mouse U251MG glioblastoma xenografts[1].
TMLZ-G46 (30 mg/kg; i.g.; once daily; 60 days) reduces tumor burden of orthotopic U251MG glioblastoma xenografts in mice and significantly prolongs their survival, with efficacy comparable to that of Temozolomide (HY-17364)[1].

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

Animal Model: BALB/c nude (male, 6-8 weeks old, subcutaneous U251MG glioblastoma xenograft model)[1]
Dosage: 60 mg/kg
Administration: p.o.; once daily; 28 days
Result: Achieved a tumor growth inhibition rate of 83.7% compared to vehicle control.
Reduced mean tumor volume and tumor weight.
Showed no significant changes in body weight, organ index (heart, liver, spleen, lung, kidney), serum AST/ALT activities, or histopathological alterations of major organs.
Reduced PCNA- and Ki67-positive tumor cells significantly.
Molecular Weight

575.74

Formula

C37H41N3O3
CAS No.
SMILES

O=C(/C(C#N)=C1C2=CC=CC=C2OC3=CC=CC=C3\1)NCCC4CCN(CC4)CC5=CC=C(C=C5)OCC6CCCCC6
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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TMLZ-G46 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:

TMLZ-G463116767-83-7ApoptosisDNA-binding domainhuman liver microsomesrat liver microsomesglioma xenograft modelsG0/G1 cell cycle arrestcytochrome P450mouse liver microsomesZNF207apoptosisSprague-Dawley ratsInhibitorinhibitorinhibit

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