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Art. -Nr.: HY-175757

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HsClpP activator-2

HsClpP activator-2 is an orally active HsClpP agonist with a K_D of 40 nM. HsClpP activator-2 potently inhibits SCLC cells including H69 (IC₅₀ = 0.17 μM) and H82 (IC₅₀ = 0.19 μM). HsClpP activator-2 disrupts mitochondrial membrane potential (MMP), as well as induces apoptosis and ROS in H82 cells. HsClpP activator-2 significantly inhibits tumor growth in non-SMC xenograft models with a tumor growth inhibition. HsClpP activator-2 can be used for the study of small cell lung carcinoma (SCLC).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₉H₂₆F₃N₃O₂
Molecular Weight:505.53

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

HsClpP activator-2 Chemical Structure

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Preis

Verfügbarkeit

Menge

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HsClpP

40 nM (Kd)

In Vitro

HsClpP activator-2 (Compound 8o) (0.02-10 μM, 72 h) shows potent antiproliferative activity against H69, H82, and non-SMC cells, with IC₅₀ values of 0.17 μM, 0.19 μM, and 0.1 μM, respectively^[1].
HsClpP activator-2 (100-400 nM, 72 h) induces dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells^[1].
HsClpP activator-2 (100-400 nM, 72 h) significantly reduces intracellular ATP levels and increases ROS levels in H82 cells in a dose-dependent manner^[1].
HsClpP activator-2 (100-400 nM, 48-72 h) disrupts mitochondrial membrane potential (MMP) and induces apoptosis in H82 cells^[1].
HsClpP activator-2 (100-400 nM, 24-48 h) inhibits colony formation and migration of non-SMC cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

H82 cells
Concentration:

100, 200, 400 nM
Incubation Time:

72 h
Result:

Induced dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC	T_1/2	F	CL	MRT
Rat^[1]	15 mg/kg	p.o.	104 ng/mL	0.5 h	370.58 ng·h/mL	3.117 h	12.2 %	/	/
Rat^[1]	5 mg/kg	i.v.	2140 ng/mL	/	1013.623 ng·h/mL	0.383 h	/	10 mL/min/kg	0.54 h

In Vivo

HsClpP activator-2 (Compound 8o) (1.3-5 mg/kg, i.p., twice weekly, 20 days) demonstrates potent anti-tumor efficacy in male BALB/c nude mice bearing non-SMC cell xenografts^[1].

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

Animal Model:

Non-SMC cells (1×10⁶ cells) were subcutaneously implanted into the flanks of 6-8-week-old male BALB/c nude mice (18-22 g)^[1]
Dosage:

1.3, 2.5, 5 mg/kg
Administration:

i.p., twice weekly, 20 days
Result:

Achieved tumor growth inhibition (TGI) rates of 37.03%, 49.12%, and 60.44% for tumor weight, as well as 41.93%, 50.08%, and 63.01% for tumor volume at doses of 1.3, 2.5, and 5 mg/kg, respectively.
Showed no significant changes in body weight and no pathological damage in major organs (heart, liver, spleen, lung, kidney).
Reduced the Ki67 expression.
Increased the Caspase 3 expression in tumor.

Chemical Information

Molecular Weight 505.53
Formel C₂₉H₂₆F₃N₃O₂
SMILES

O=C(C1=C(C2=CC=C(CO)C=C2)CCN(CC3=CC=CC(C#N)=C3)C1)NCC4=CC=C(C(F)(F)F)C=C4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[1]. Li L, et al. A shape complementarity strategy based on NCA029 enables potent HsClpP agonists for the treatment of small cell lung carcinoma. Eur J Med Chem. 2025 Dec 5;299:118008. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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