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Burden

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (2) Apoptosis (8) Bacterial (4) Bcl-2 Family (1) Calcium Channel (1) Cannabinoid Receptor (1) Carbonic Anhydrase (1) Ceramidase (1) Eukaryotic Initiation Factor (eIF) (2) FLT3 (1) Fungal (1) Galectin (1) Histone Methyltransferase (3) JAK (1) LPL Receptor (1) Parasite (6) PERK (1) Radionuclide-Drug Conjugates (RDCs) (2) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (1) Infection (12) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

MCE Kits

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-162066

DNDI-6174	Parasite	Infection
DNDI-6174 is a cytochrome bc1 complex inhibitor with potent in vitro activity against a variety of Leishmania species. DNDI-6174 can reduce parasite burden in animal models of infection .

HY-148422

Rohinitib	Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .

HY-145441

GEM–IB	Others	Cancer
GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS) .

HY-163342

Antibacterial agent 190	Bacterial	Infection
Antibacterial agent 190 (compound 16) is a antibacterial agent. Antibacterial agent 190 shows antibacterial activity. Antibacterial agent 190 reduces the bacterial burden of the peritoneum and blood .

HY-P10761

DPI-4452	Radionuclide-Drug Conjugates (RDCs) Carbonic Anhydrase	Cancer
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and therapy. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC₅₀ for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models .

HY-160078

Deferiprone O-β-D-glucuronide	Others	Metabolic Disease
Deferiprone O-β-D-glucuronide is a novel orally active iron chelator. Deferiprone O-β-D-glucuronide shows the capability of reducing the iron burden in patients with β-thalassemia .

HY-146190

Callophycin A	Bacterial Antibiotic	Infection Inflammation/Immunology
Callophycin A, a red seaweed derived metabolite, possessing potent activity against *Candida albicans* with MIC of 62.5~250 mg/L. Callophycin A significantly reduces fungal burden of vaginal candidiasis induced mice, also decreases inflammatory response and immune molecules .

HY-151484

Anti-infective agent 4	Parasite	Infection
Anti-infective agent 4 (compound 73) is an orally active inhibitor of *Trypanosoma cruzi* with an IC₅₀ value of 0.016 μM. Anti-infective agent 4 effectively reduces parasite burden in vivo. Anti-infective agent 4 can be used for the research of infection .

HY-151485

Anti-infective agent 5	Parasite	Infection
Anti-infective agent 5 (compound 74) is an orally active inhibitor of *Trypanosoma cruzi* with an IC₅₀ value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection .

HY-P10057

cpm-1285	Apoptosis	Cancer
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC₅₀ value of 130 nM. cpm-1285 reduces tumor burden in mice .

HY-145741

MptpB-IN-1	Antibiotic	Infection
MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacterium tuberculosis survival and infection burden .

HY-123410

KM-233	Cannabinoid Receptor	Cancer
KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research .

HY-145690

HP1328	FLT3	Cancer
HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia .

HY-151925

Antibacterial agent 126	Bacterial	Infection
Antibacterial agent 126 is a potent antibacterial agent. Antibacterial agent 126 reduces the burden of biofilm to avoid developing agent resistance. Antibacterial agent 126 disturbs the membrane integrity and leads to the leakage of intracellular materials. Antibacterial agent 126 increase in ROS and reactive nitrogen species (RNS) production .

HY-101991

ML291	PERK Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden .

HY-W064657

Momelotinib dihydrochloride	JAK	Others
Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis .

HY-141429

AS-99 free base	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-141429C

AS-99	Histone Methyltransferase Apoptosis	Cancer
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-146079

Antifungal agent 31	Fungal	Infection
Antifungal agent 31 (compound 12) is a potent and orally active triazole antifungal agents with a pyrrolotriazinone scaffold. Antifungal agent 31 shows antifungal activity against Candida spp. and filamentous fungi. Antifungal agent 31 significantly reduced mortality rates and kidney fungal burden in two murine models of lethal systemic infections .

HY-147865

Apoptosis inducer 8	Galectin Apoptosis	Cancer
Apoptosis inducer 8 (Compound 7c) is a galectin-1 (gal-1) mediated apoptosis-inducing agent against global major leading lung cancer burden. Apoptosis inducer 8 significantly reduced the gal-1 protein level. Apoptosis inducer 8 is also a PET imaging agent .

HY-141429A

AS-99 TFA 1 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .

HY-P10559

(RXR)4XB	Bacterial	Infection
(RXR)4XB is a cell-penetrating peptide, that binds the phosphorodiamidate morpholino oligomers (PMOs), forms peptide-conjugated PMOs (PPMOs), and improves the delivery of PMO into bacterial cells. (RXR)4XB-PMO conjugate prevents the formation of biofilms, inhibits Pseudomonas aeruginosa with MIC₅₀ of 0.5 to 16 μM, and reduces the bacterial burden in mouse acute pneumonia models .

HY-100740A

Lanabecestat hydrochloride AZD-3293 hydrochloride; LY3314814 hydrochloride	Others	Neurological Disease
Lanabecestat (AZD-3293) hydrochloride is a potent BACE1 inhibitor that has been investigated for its potential as a modifying treatment for Alzheimer's disease. Lanabecestat (hydrochloride) demonstrated significant dose- and time-dependent reductions in concentrations of amyloid beta peptides in plasma, cerebrospinal fluid, and brain. Lanabecestat (hydrochloride) was also shown to produce reductions in Aβ neuritic plaque burden without demonstrating clinical benefits or slowing the progression of Alzheimer's disease pathophysiology.

HY-14744B

Levamlodipine hydrochloride (S)-Amlodipine hydrochloride; Levoamlodipine hydrochloride	Calcium Channel	Cardiovascular Disease
Levamlodipine hydrochloride (Levoamlodipine hydrochloride) is a dihydropyridine calcium channel blocker. Levamlodipine hydrochloride reduces the inflow of calcium ions by blocking L-type calcium channels on vascular smooth muscle cells, thereby leading to vasodilation, lower blood pressure and lighten the burden on the heart. Levamlodipine hydrochloride has activity to lower blood pressure and relieve angina. The binding properties of Levamlodipine hydrochloride to human serum albumin (HSA) contribute to the study of drug transport and release mechanisms in the body .

HY-121495

BKI-1369	Parasite	Infection
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC₅₀ of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .

HY-P9983

Lintuzumab HuM-195	Others Radionuclide-Drug Conjugates (RDCs) Transmembrane Glycoprotein	Inflammation/Immunology
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR? and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .

HY-124623

DNDI-8219	Parasite	Infection
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.

HY-155520

Antileishmanial agent-19	Parasite	Infection
Antileishmanial agent-19 (Compound F27) is an antileishmanial agent, with a IC₅₀ of 3.39 μM for L. donovani promastigotes. Antileishmanial agent-19 inhibits Leishmania prolyl-tRNA synthetase. Antileishmanial agent-19 inhibits host PI3K/Akt/CREB axis-mediated IL-10 secretion. Antileishmanial agent-19 induces autophagy-mediated apoptosis in L. donovani promastigotes. Antileishmanial agent-19 reduces parasite burden in L.d-infected animals .

HY-158783

SACLAC	Ceramidase Bcl-2 Family LPL Receptor Apoptosis	Neurological Disease
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a K_i of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .

HY-114162B

VTP50469 mesylate	Others	Cancer
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.

Cat. No.	Product Name

HY-L073

Anti-Hepatitis C Virus Compound Library	327 compounds
Hepatitis C virus (HCV) is a hepatotropic enveloped positive- strand RNA virus (family Flaviviridae) that infects the parenchymal cells of the liver. HCV infection is a significant public health burden. Globally, an estimated 71 million people have chronic hepatitis C virus infection. A significant number of those who are chronically infected will develop cirrhosis or liver cancer. To date, there is no vaccine against HCV, and combination pegylated alpha interferon (pIFN-) and ribavirin, the main standard-of-care treatment for HCV, is effective in only a subset of patients and is associated with a wide spectrum of toxic side effects and complications. More recently, new therapeutic approaches that target essential components of the HCV life cycle have been developed, including direct-acting antiviral (DAA) that specifically block a viral enzyme or functional protein and host-targeted agents (HTA) that block interactions between host proteins and viral components that are essential to the viral life cycle. However, the genetic diversity of HCV viruses and the stage of liver disease (i.e., cirrhosis) are revealing themselves as obstacles for effective, pan-genotypic treatments. There still exists a need for the discovery and development of new HCV inhibitors. In particular, since the future of HCV therapy will likely consist of a cocktail approach using multiple inhibitors that target different steps of infection, new antivirals targeting all steps of the viral infection cycle. MCE offers a unique collection of 327 compounds with identified and potential anti-HCV activity. MCE Anti- Hepatitis C Virus Compound Library is a useful tool for discovery new anti-HCV drugs and other anti-infection research.

Anti-Hepatitis C Virus Compound Library

327 compounds

Hepatitis C virus (HCV) is a hepatotropic enveloped positive- strand RNA virus (family Flaviviridae) that infects the parenchymal cells of the liver. HCV infection is a significant public health burden. Globally, an estimated 71 million people have chronic hepatitis C virus infection. A significant number of those who are chronically infected will develop cirrhosis or liver cancer. To date, there is no vaccine against HCV, and combination pegylated alpha interferon (pIFN-) and ribavirin, the main standard-of-care treatment for HCV, is effective in only a subset of patients and is associated with a wide spectrum of toxic side effects and complications. More recently, new therapeutic approaches that target essential components of the HCV life cycle have been developed, including direct-acting antiviral (DAA) that specifically block a viral enzyme or functional protein and host-targeted agents (HTA) that block interactions between host proteins and viral components that are essential to the viral life cycle. However, the genetic diversity of HCV viruses and the stage of liver disease (i.e., cirrhosis) are revealing themselves as obstacles for effective, pan-genotypic treatments. There still exists a need for the discovery and development of new HCV inhibitors. In particular, since the future of HCV therapy will likely consist of a cocktail approach using multiple inhibitors that target different steps of infection, new antivirals targeting all steps of the viral infection cycle.

MCE offers a unique collection of 327 compounds with identified and potential anti-HCV activity. MCE Anti- Hepatitis C Virus Compound Library is a useful tool for discovery new anti-HCV drugs and other anti-infection research.

Cat. No.	Product Name	Target	Research Area

HY-P10761

DPI-4452	Radionuclide-Drug Conjugates (RDCs) Carbonic Anhydrase	Cancer
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and therapy. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC₅₀ for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models .

HY-P10057

cpm-1285	Apoptosis	Cancer
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC₅₀ value of 130 nM. cpm-1285 reduces tumor burden in mice .

HY-P10559

(RXR)4XB	Bacterial	Infection
(RXR)4XB is a cell-penetrating peptide, that binds the phosphorodiamidate morpholino oligomers (PMOs), forms peptide-conjugated PMOs (PPMOs), and improves the delivery of PMO into bacterial cells. (RXR)4XB-PMO conjugate prevents the formation of biofilms, inhibits Pseudomonas aeruginosa with MIC₅₀ of 0.5 to 16 μM, and reduces the bacterial burden in mouse acute pneumonia models .

MEM Non-essential Amino Acid Solution (100×)
MEM Non-essential Amino Acid Solution (100×) has been filtered and can be used directly. It adds nutrients and reduces the biosynthetic burden on cell in vitro.

Cat. No.	Product Name	Target	Research Area

HY-P9983

Lintuzumab HuM-195	Inhibitory Antibodies Radionuclide-Drug Conjugates (RDCs) Transmembrane Glycoprotein	Inflammation/Immunology
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR? and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .

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