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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
14 Results for "
HsClpP
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "HsClpP" in MCE Product Catalog:
1
1 Cited Publications
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ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
Cat. No.: HY-163319
CAS No.: 3032667-94-7
NCA029 is a potent and selective homo sapiens caseinolytic protease P (HsClpP) activator with an EC50 of 0.15 μM. NCA029 acts on HsClpP to activate an ATF3-dependent integrative stress response, leading to colon cancer cell death .
Cat. No.: HY-162650
CAS No.: 3054715-45-3
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 .
Cat. No.: HY-173048
CAS No.: 3104462-62-3
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CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
Cat. No.: HY-176427
CAS No.: 3087033-83-5
HsClpP activator-1 (compound 24) is a potent HsClpP activator with an EC50 of 0.22 μM. HsClpP activator-1 effectively inhibits cancer cell growth with IC50 values of 0.1-1 μM .
Cat. No.: HY-175757
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HsClpP activator-2 is an orally active HsClpP agonist with a KD 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) .
Cat. No.: HY-162462
CAS No.: 3036751-77-3
Antitumor agent-151 (7k) is a significant HsClpP agonist and an antileukemia drug candidate. Antitumor agent-151 (7k) exhibits remarkably enhanced proteolytic activity of HsClpP (EC50 = 0.79 μM) and antitumor activity in vitro (IC50 = 0.038 μM). Antitumor agent-151 (7k) induces apoptosis .
Cat. No.: HY-184944
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HsClpP-ligand-1 is an intermediate derived from HsClpP ligands, and also serves as an HsClpP recruitment module for constructing mitochondria-targeted pan-PDK degraders. HsClpP-ligand-1 acts as the HsClpP ligand of the bifunctional degrader Pan-PDK degrader-1 (HY-184943) .
Cat. No.: HY-181934
CAS No.: 3125957-10-7
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ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd 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 .
Cat. No.: HY-184945
CAS No.: 252016-13-0
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PDK ligand-1 (Compound 16) is a target protein ligand that serves as an HsClpP recruitment module for constructing mitochondrially targeted pan-PDK degraders. PDK ligand-1 can be used for the synthesis of Pan-PDK degrader-1 (HY-184943) .
Cat. No.: HY-184943
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Pan-PDK degrader-1 is a pan-PDK class PROTAC degrader that degrades PDK2, PDK3 and PDK4 with DC50 values of 9.2 nM, 9.9 nM and 11.5 nM, respectively. Pan-PDK degrader-1 recruits the mitochondrial protease HsClpP and induces selective pan-PDK degradation via HsClpP-mediated proteolysis. Pan-PDK degrader-1 reprograms mitochondrial metabolism toward oxidative phosphorylation, promoting ROS accumulation, mitochondrial permeability transition pore opening, endogenous mitochondrial apoptosis, calreticulin exposure and HMGB1 release. Pan-PDK degrader-1 upregulates cleaved Caspase-9, Caspase-3 and PARP. Pan-PDK degrader-1 inhibits primary and distal tumor growth via selective degradation of PDK in tumor tissues. Pan-PDK degrader-1 can be used for the research of breast cancer .
Cat. No.: HY-186109
CAS No.: 2999673-51-5
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ZY39 is a SaClpP agonist. ZY39 promotes the enzymatic hydrolysis of SaClpP and HsClpP in vitro. ZY39 inhibits the growth of Staphylococcus aureus strains. ZY39 reduces the load of Staphylococcus aureus in organs and ascites in mouse peritonitis models and zebrafish infection models, and improves the survival rate of model animals. ZY39 can be used in studies related to Staphylococcus aureus infection, such as peritonitis .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
