ClpP Inhibitor

Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC₅₀ value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.

(3R,4R)-A2-32-01 (compound 24(R,R)), the (R,R)-enantiomer of A2-32-01, is a Staphylococcus aureus caseinolytic protease (SaClpP) inhibitor.

Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC₅₀ of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways.

(3S,4S)-A2-32-01 (compound 24(S,S)), a less active (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protein proteases (ClpP) inhibitor.

SL44 is an agonist for human caseinolytic protease P (HsClpP), with an EC₅₀ of 1.30 μM. SL44 inhibits the proliferation of LM3 with an IC₅₀ of 3.1 μM. SL44 induces apoptosis in HCC cells, through the degradation of respiratory chain complex subunits. SL44 exhibits antitumor efficacy in mouse models without obvious toxicity (LD₅₀=400 mg/kg). SL44 exhibits good pharmacokinetic characters in rat models.

Z-GGF-CMK is an Antibacterial agent, an inhibitor of the ClpP1P2 serine protease complex (with an IC₅₀ of 50 μM against intracellular ClpP1P2 protease activity in Mycobacterium bovis BCG), and a selective inhibitor of the mycobacterial Proteasome (with an IC₅₀ of 50 μM against the proteasome in M. bovis BCG). Z-GGF-CMK inhibits the growth of mycobacteria. Z-GGF-CMK exhibits cytotoxic activity against liver cancer cells. Z-GGF-CMK can be used in the research of tuberculosis.

(S)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC₅₀ of 1.4 μM.

(R)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC₅₀ of 1.5 μM. (R)-ZG197 also activates Homo sapiens ClpP (HsClpP) with an EC₅₀ of 31.4 μM.

ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model.

ClpP1P2-IN-1 is a protease inhibitor targeting ClpP1P2 of Mycobacterium tuberculosis, with a K_i value of 0.04 μM. ClpP1P2-IN-1 inhibits the growth of Mycobacterium tuberculosis and shows low cytotoxicity against mammalian kidney cells. ClpP1P2-IN-1 can be used in the research of tuberculosis.

ClpP agonist 1 is a Staphylococcus aureus ClpP (SaClpP) agonist with an EC₅₀ of 1.44 μM, K_d values of 2.95 μM (isothermal titration calorimetry) and 18 μM (bio-layer interferometry), and a low drug resistance frequency. ClpP agonist 1 reduces bacterial load, shrinks infected area and improves histopathological outcomes in a mouse skin infection model. ClpP agonist 1 can be used for the research of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) skin infections.

Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.

Tamarixetin (Standard) is the analytical standard of Tamarixetin. This product is intended for research and analytical applications. Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC₅₀ of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways.