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製品番号: HY-181934

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ClpP activator-2

ClpP activator-2 (Compound GU18) is a ClpP activator with a K_d of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC₅₀ of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity.

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CAS 番号: 3036751-71-7
分子式: C₂₂H₁₉Cl₂F₃N₄O
分子量:483.31

保管条件:

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

ClpP activator-2 構造式

CAS 番号: 3036751-71-7

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- Parmacokinetics
- 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

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	10 μM Compound: 7e	Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]

体外実験

ClpP activator-2 potently activates purified HsClpP with an EC₅₀ of 0.54 ± 0.12 μM^[1].
ClpP activator-2 (2 h) promotes the degradation of α-casein by HsClpP, with an EC₅₀ of 1.09 ± 0.08 μM^[1].
ClpP activator-2 binds to purified HsClpP, and its dissociation constant K_d is determined as 5.01 ± 1.05 μM by ITC^[1].
ClpP activator-2 (0.45 μM; 24 h) causes significant mitochondrial ultrastructural damage to AMO.1 MM cells after treatment at 0.45 μM for 24 h^[1].
ClpP activator-2 (0.15-0.6 μM; 48 h) promotes the accumulation of mitochondrial reactive oxygen species (ROS) in AMO.1 and ARP1 multiple myeloma (MM) cells in a concentration-dependent manner after 48 h of treatment^[1].

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

Cell Viability Assay^[1]

Cell Line:

Human multiple myeloma cell lines AMO.1, ARP1
Concentration:

Gradient concentrations
Incubation Time:

24 h, 48 h, 72 h
Result:

Reduced cell viability in a time- and concentration-dependent manner.
For AMO.1 cells, reached IC₅₀ values of 1.30 ± 0.08 μM (24 h), 0.68 ± 0.03 μM (48 h), and 0.08 ± 0.01 μM (72 h).
For ARP1 cells, reached IC₅₀ values of 1.81 ± 0.14 μM (24 h), 0.86 ± 0.08 μM (48 h), and 0.21 ± 0.02 μM (72 h).

Cell Cycle Analysis^[1]

Cell Line:

Human multiple myeloma cell lines AMO.1, ARP1
Concentration:

0.15-0.6 μM
Incubation Time:

24 h
Result:

Induced dose-dependent G1 phase.

Apoptosis Analysis^[1]

Cell Line:

Human multiple myeloma cell lines AMO.1, ARP1
Concentration:

0.15-0.6 μM (apoptosis assay); 0.45 μM (Western blotting)
Incubation Time:

24 h, 48 h, 72 h (apoptosis assay); 48 h (Western blotting)
Result:

Induced time- and concentration-dependent apoptosis, with 95% of AMO.1 cells and 73.8% of ARP1 cells apoptotic after 72 h of 0.6 μM treatment.
Upregulated cleaved caspase-3.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	Bioavailability
Rat^[1]	5 mg/kg	i.v.	16733.33 ng/mL	3.854 h	38.9 %
Rat^[1]	10 mg/kg	p.o.	6050 ng/mL	3.198 h	/

体内実験

ClpP activator-2 (5-30 mg/kg; i.p.; once every other day; 14 days) dose-dependently inhibits the tumor growth of multiple myeloma in NOD/SCID mice^[1].

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

Animal Model:

NOD/SCID (female, 6-8 weeks old, subcutaneous xenograft model)^[1]
Dosage:

5 mg/kg; 15 mg/kg; 30 mg/kg
Administration:

i.p.; every other day; 14 days
Result:

Achieved 56.7% tumor volume inhibition at 5 mg/kg.
Achieved 83.4% tumor volume inhibition at 15 mg/kg.
Achieved 91.4% tumor volume inhibition at 30 mg/kg.
Showed no treatment-related damage to major organs in the 30 mg/kg group compared to controls.

化学情報

CAS 番号 3036751-71-7
分子量 483.31
分子式 C₂₂H₁₉Cl₂F₃N₄O
SMILES

O=C1NC(NCC2=CC=C(C(F)(F)F)C=C2)=NC3=C1CN(CC3)CC4=CC(Cl)=C(Cl)C=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Liu X, et al. Discovery of 2-(methylamino)-5,6,7,8-tetrahydropyrido[4,3-d] pyrimidine derivatives as novel HsClpP activators for multiple myeloma therapy. Eur J Med Chem. Published online February 26, 2026. [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.

100 mg

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