1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. LZL50

LZL50 is an orally effective human caseinolytic protease P (hClpP) activator with an EC50 of 0.29 μM. LZL50 activates hClpP, a serine protease that mediates mitochondrial quality control by degrading damaged or misfolded mitochondrial proteins. LZL50 exhibits antitumor activity in a breast cancer xenograft mouse model. LZL50 can be used in research related to breast cancer.

For research use only. We do not sell to patients.

LZL50

LZL50 Chemical Structure

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Description

LZL50 is an orally effective human caseinolytic protease P (hClpP) activator with an EC50 of 0.29 μM. LZL50 activates hClpP, a serine protease that mediates mitochondrial quality control by degrading damaged or misfolded mitochondrial proteins. LZL50 exhibits antitumor activity in a breast cancer xenograft mouse model. LZL50 can be used in research related to breast cancer[1].

In Vitro

LZL50 (5 nM-30 μM; 72 h) inhibits the growth of MDA-MB-231 cells with an IC50 of 0.30 ± 0.04 μM after 72 h of treatment[1].
LZL50 (1.0 μM; up to 120 min) has moderate metabolic stability in human liver microsomes, with a CLint of 46.2 mL/min/kg and a T1/2 of 39 min[1].

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

Parmacokinetics
Species Dose Route Cmax Tmax AUC0-t AUC0-∞ T1/2
Rat[1] 15 mg/kg p.o. 1939.24 ng/mL 1.12 h 18403.92 ng·h/mL 19010.67 ng·h/mL 4.37 h
In Vivo

LZL50 (5-20 mg/kg; p.o.; daily; 15 days) demonstrates potent dose-dependent in vivo antitumor activity in MDA-MB-231 xenografted mice[1].

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

Animal Model: BALB/c nude (female, 5 weeks old)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: p.o.; daily; 15 days
Result: Nearly completely suppressed tumor growth at 20 mg/kg.
Showed no significant body weight loss in any treatment group during the 15-day treatment period.
Molecular Weight

555.61

Formula

C31H33F4N3O2

SMILES

O=C1N([C@H](CC2=CC=C(C=C21)CC3=CC=C(C=C3)F)COCCN4CCNCC4)CC5=CC=C(C=C5)C(F)(F)F

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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
References
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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.

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Product Name:
LZL50
Cat. No.:
HY-181764
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