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Results for "

20s proteasome Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (20) Akt (1) Apoptosis (8) Autophagy (6) Deubiquitinase (1) Endogenous Metabolite (1) Mitophagy (1) MMP (1) NF-κB (3) Parasite (2) ROS Kinase (1)
By Research Areas:	Cancer (20) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (4) Neurological Disease (2)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Proteasome

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-139331

20S Proteasome-IN-1	Proteasome	Neurological Disease Inflammation/Immunology Cancer
20S Proteasome-IN-1 is a 26S proteasome inhibitor extracted from patent WO2006128196A2 compound 2. 20S Proteasome-IN-1 has the potential for cancer, immune-related disorders, inflammation, ischemic conditions, neurodegenerative disorders and other diseases research .

HY-151195

20S Proteasome-IN-4	Proteasome Parasite	Infection
20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active **20S proteasome** inhibitor with an IC₅₀ of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT) .

HY-150590

20S Proteasome-IN-2	Proteasome	Cancer
20S Proteasome-IN-2 is a human **20S proteasome** inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC₅₀ of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .

HY-150591

20S Proteasome-IN-3

Proteasome Cancer

20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC₅₀=1.64 μM) . 20S Proteasome-IN-3 shows anti-tumor proliferation activity .

20S Proteasome-IN-3	Proteasome	Cancer
20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC₅₀=1.64 μM) . 20S Proteasome-IN-3 shows anti-tumor proliferation activity .

HY-158150

20S Proteasome-IN-5	Proteasome	Cancer
20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the **20S Proteasome, with IC₅₀** values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .

HY-W054146

RAMB4 1 Publications Verification	Proteasome	Cancer
RAMB4 is a *ubiquitin-proteasome* system (UPS)-stressor*. RAMB4 inhibits* ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .

HY-13067

Celastrol 30+ Cited Publications Tripterine; Tripterin	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite	Inflammation/Immunology Cancer
Celastrol (Tripterine;Tripterin) is a *proteasome* inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified **20S proteasome with IC₅₀** of 2.5 μM.

HY-10453

Ixazomib 10+ Cited Publications MLN2238	Proteasome Autophagy	Cancer
Ixazomib (MLN2238) is a selective, potent, and reversible *proteasome* inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

HY-10452

Ixazomib citrate 4 Publications Verification MLN9708	Proteasome Autophagy	Cancer
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the **20S proteasome with an IC₅₀ of 3.4 nM and a K_i** of 0.93 nM.

HY-108552

MG-115 1 Publications Verification	Proteasome Apoptosis	Cancer
MG-115 is a potent and reversible *proteasome* inhibitor, with K_is of 21 nM and 35 nM for *20S* and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis .

HY-N2117

Isoginkgetin 10+ Cited Publications	MMP Akt NF-κB Proteasome Apoptosis Autophagy	Inflammation/Immunology Cancer
Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the **20S proteasome, induces apoptosis and activates autophagy** .

HY-10227

Bortezomib Maximum Cited Publications 122 Publications Verification PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib (PS-341) is a reversible and selective *proteasome* inhibitor, and potently inhibits **20S proteasome (K_i*=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits* NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .

HY-113824

RID-F Ridaifen-F	Proteasome	Cancer
RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic *proteasome* inhibitor. RID-F inhibits human 20S proteasome activity, with IC₅₀s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively .

HY-107412

Proteasome inhibitor IX PS-IX; AM114	Proteasome	Cancer
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 ^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .

HY-149514

BC-05	Proteasome	Cancer
BC-05 is an orally active and potent inhibitor of CD13 and *proteasome. BC-05 has an IC₅₀* value of 0.13 μM for human CD13 and an IC₅₀ value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research .

HY-150226

Enzyme-IN-1	Proteasome	Inflammation/Immunology
Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the **20S proteasome**. Enzyme-IN-1 may has potential antiinflammatory properties .

HY-135396

(1S,2S)-Bortezomib	Proteasome Apoptosis	Cancer
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective *proteasome* inhibitor, and potently inhibits **20S proteasome (K_i** of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans .

HY-10227S

Bortezomib-d8 PS-341-d₈; LDP-341-d₈; NSC 681239-d₈	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Proteasome	Cancer
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, *pan-proteasome* inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-N2166

Tomatine α-Tomatine; Lycopersicin; Tomatin
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits **20S proteasome** activity .

HY-153034

LONP1-IN-2	Others	Cancer
LONP1-IN-2 (compound 9d) is a potent and selective LONP1 inhibitor with IC₅₀ values of 0.187 μM and >10 μM for LONP1 and 20S proteasome, respectively. LONP1-IN-2 can be used in research of cancer .

HY-136528

RA-9	Deubiquitinase Apoptosis	Cancer
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .

HY-16594

Lactacystin 2 Publications Verification	Proteasome Apoptosis ROS Kinase	Infection Cardiovascular Disease Neurological Disease Cancer
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S *proteasome* inhibitor (IC₅₀ = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on ^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7] ^[8] ^[9] ^[10].

HY-161079

TDI-8304	Parasite	Infection
TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent **Plasmodium falciparum (Pf20S)** inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .

20S Proteasome-IN-5	Proteasome	Cancer
20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the **20S Proteasome, with IC₅₀** values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13067

Celastrol Maximum Cited Publications 31 Publications Verification Tripterine; Tripterin	Triterpenes Structural Classification Classification of Application Fields Anti-aging Terpenoids Source classification Celastraceae Plants Tripterygium wilfordii Hook. f. Inflammation/Immunology Disease Research Fields Cancer	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite
Celastrol (Tripterine;Tripterin) is a *proteasome* inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified **20S proteasome with IC₅₀** of 2.5 μM.

HY-N2117

Isoginkgetin 10+ Cited Publications	Structural Classification Flavonoids Ginkgoaceae Classification of Application Fields Source classification Phenols Polyphenols Plants Biflavones Ginkgo biloba Disease Research Fields Cancer	MMP Akt NF-κB Proteasome Apoptosis Autophagy
Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the **20S proteasome, induces apoptosis and activates autophagy** .

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Marine natural products Source classification Marine microorganism	Proteasome
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, *pan-proteasome* inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-16594

Lactacystin 2 Publications Verification	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Proteasome Apoptosis ROS Kinase
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S *proteasome* inhibitor (IC₅₀ = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on ^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7] ^[8] ^[9] ^[10].

Cat. No.	Product Name	Chemical Structure

HY-10227S

Bortezomib-d8
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

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20s proteasome Inhibitors

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products