Search Result
Results for "
overexpress
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-101280
-
|
NAMPT
|
Cancer
|
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
-
- HY-P2508
-
|
Mucin
|
Cancer
|
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .
|
-
-
- HY-162470
-
|
Aurora Kinase
|
Cancer
|
DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
|
-
-
- HY-100111
-
GLX351322
Maximum Cited Publications
31 Publications Verification
|
NADPH Oxidase
|
Metabolic Disease
|
GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μM.
|
-
-
- HY-135336
-
(R)-(+)-Verapamil hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents .
|
-
-
- HY-101280A
-
|
NAMPT
|
Cancer
|
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
-
- HY-163919
-
|
Topoisomerase
|
Cancer
|
N,N-Dimethyl-idarubicin-trisaccharide (compound 26) is an efficient intercalating agent. N,N-Dimethyl-idarubicin-trisaccharide shows excellent cytotoxicity against ABCG2-overexpressing and ABCB1-overexpressing cells with IC50s of 19 and 32 nM, respectively .
|
-
-
- HY-149389
-
|
Others
|
Endocrinology
|
PNMT-IN-1 (inhibtor 4) is a specific inhibitor of phenylethanolamine N-methyltransferas (PNMT) with a Ki value of 1.2 nM and a IC50 value of 81 nM.
PNMT-IN-1 also inhibits the vitality of DNMT1 and DNMT3b, with the IC50 value of 61 μM and 17 μM, respectively, and has an antagonistic effect on epinephrine.PNMT-IN-1 (inhibtor 4 ) is a second generation inhibitor .
|
-
-
- HY-P10328
-
|
DNA/RNA Synthesis
|
Metabolic Disease
|
Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
|
-
-
- HY-P99630
-
MM-302
|
EGFR
|
Cancer
|
Gancotamab (MM-302) is a HER2-targeted antibody-liposomal Doxorubicin conjugate with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells .
|
-
-
- HY-156244
-
|
PROTACs
|
Cancer
|
PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models .
|
-
-
- HY-135336S
-
(R)-(+)-Verapamil-d7 hydrochloride
|
Isotope-Labeled Compounds
P-glycoprotein
Apoptosis
|
Cancer
|
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
|
-
-
- HY-163918
-
|
Others
|
Cancer
|
N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells .
|
-
-
- HY-156418
-
|
DNA/RNA Synthesis
|
Cancer
|
KY386 is a potent, selective inhibitor of DHX33 helicase, with the IC50 of 19 nM. KY386 inhibits U251-MG cells (DHX33-overexpressing cancer cell strain) with IC50 of 20 nM.and shows potent anti-cancer activity and moderate metabolic stability .
|
-
-
- HY-156243
-
|
Others
|
Cancer
|
GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models .
|
-
-
- HY-107760
-
-
-
- HY-169244
-
|
CDK
Bcl-2 Family
|
Cancer
|
CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells .
|
-
-
- HY-107760A
-
-
-
- HY-158828
-
|
EGFR
|
Cancer
|
SSO111 sodium, a 20mer fully modified antisense oligonucleotide, targets the oncogene?HER2. SSO111 sodium induces exon 15 skipping during splicing, leading to the generation of a novel mRNA transcript that excludes exon 15. SSO111 sodium downregulated HER2 mRNA, which resulted in the inhibition of proliferation and induction of apoptosis in HER2-overexpressing tumor cells.
|
-
-
- HY-10822A
-
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
|
-
-
- HY-100416A
-
|
GlyT
|
Neurological Disease
|
LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a .
|
-
-
- HY-100416
-
|
GlyT
|
Neurological Disease
|
LY2365109 is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a .
|
-
-
- HY-156863
-
|
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
|
GRK2 Inhibitor 2 (Compound 8h) is a GRK2 inhibitor (IC50: 19 nM). GRK2 Inhibitor 2 also inhibits Aurora-A (IC50: 137 nM). GRK2 Inhibitor 2 promotes β-AR-mediated cAMP accumulation in GRK2-overexpressed HEK293 cells. GRK2 Inhibitor 2 can be used for research of congestive heart failure (HF) .
|
-
-
- HY-50883
-
|
γ-secretase
|
Neurological Disease
|
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
|
-
-
- HY-157942
-
|
Cytochrome P450
|
Cancer
|
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
|
-
-
- HY-12425
-
-
-
- HY-132934
-
|
BCRP
|
Cancer
|
Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in the
BCRP-overexpressed HEK293/R2 cells.
|
-
-
- HY-115831
-
S1P1 agonist 3
|
LPL Receptor
|
Cardiovascular Disease
|
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .
|
-
-
- HY-100395
-
|
Apoptosis
|
Cancer
|
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
|
-
-
- HY-N2103
-
|
P-glycoprotein
|
Cancer
|
Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells .
|
-
-
- HY-10822
-
BGC 945; ONX-0801
|
Thymidylate Synthase
|
Others
|
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
|
-
-
- HY-149835
-
|
Fluorescent Dye
|
Others
|
TTX-P is a fluorescent probe. TTX-P responds in situ to the overexpressed alkaline phosphatase (ALP) in liver, imaging of diabetic liver injury in the near-infrared second-window (NIR-II) region .
|
-
-
- HY-153889
-
|
Others
|
Neurological Disease
|
BTA-EG4 is a catalase-amyloid interaction inhibitor, which can significantly enhance the neurotoxicity of amyloid peptides in catalase-overexpressing neuronal cells, and can be used in the study of neurodegenerative diseases .
|
-
-
- HY-136626
-
Cbz-Ala-Ala-Asn-AMC
|
Fluorescent Dye
|
Cancer
|
Z-Ala-Ala-Asn-AMC (Cbz-Ala-Ala-Asn-AMC) is the legumain substrate. Overexpressed legumain in 293 HEK-Leg cells potently cleaved CBZ-Ala-Ala-Asn-AMC .
|
-
-
- HY-16191
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
|
-
-
- HY-158025
-
|
DNA/RNA Synthesis
|
Cancer
|
Anticancer agent 198 (compound 18b) is a potent anticancer agent and potential WRN protein inhibitor. Anticancer agent 198 was significantly toxic to K562 cells and WRN-overexpressing PC3 cells .
|
-
-
- HY-33299
-
BTCA
|
Biochemical Assay Reagents
|
Cancer
|
Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
|
-
-
- HY-P9907
-
Anti-Human HER2, Humanized Antibody
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
ADC Antibody
|
Cancer
|
Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
-
- HY-P9907A
-
Anti-Human HER2, Humanized Antibody (PBS)
|
ADC Antibody
EGFR
|
Cancer
|
Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
-
- HY-157483
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 18 (compound 6G) is a potent inhibitor of P-gp. P-gp inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .
|
-
-
- HY-147637
-
|
Ephrin Receptor
|
Cancer
|
EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation .
|
-
-
- HY-P99516
-
HLX-06
|
VEGFR
|
Cancer
|
Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells .
|
-
-
- HY-146393
-
|
PROTACs
Cytochrome P450
|
Cancer
|
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
|
-
-
- HY-155758
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
-
- HY-155763
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
-
- HY-114877
-
|
Phosphatase
|
Cancer
|
CG-707 inhibits phosphatase of regenerating liver-3 (PRL-3) enzymatic activity with an IC50 value of 0.8 μM. CG-707 inhibits the migration and invasion of PRL-3 overexpressing colon cancer cells .
|
-
-
- HY-N144114
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300) .
|
-
-
- HY-P99153
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MORAb-003
|
Antibiotic
|
Cancer
|
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
|
-
-
- HY-142118A
-
AP 12009 sodium
|
TGF-beta/Smad
|
Cancer
|
Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
|
-
-
- HY-109050
-
GS-5829
|
Epigenetic Reader Domain
|
Cancer
|
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .
|
-
- HY-12762
-
QS11
1 Publications Verification
|
Others
|
Cancer
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
|
-
- HY-142118
-
AP 12009
|
TGF-beta/Smad
|
Cancer
|
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
|
-
- HY-138084
-
|
Separase
|
Cancer
|
SIC5-6 is a potent Separase inhibitor. Separase, a large cysteine protease, involves in chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, spindle stabilization and elongation. Separase is highly overexpressed in many solid cancers, serves as an attractive chemotherapeutic target .
|
-
- HY-162318
-
|
c-Myc
|
Cancer
|
MYC degrader 1 (compound A80.2HCl) is an orally available MYC degrader with antitumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC over-expressing cancer cells to CDK4/6 inhibitors .
|
-
- HY-N3028
-
|
Microtubule/Tubulin
|
Cancer
|
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM .
|
-
- HY-125835
-
CP-10
1 Publications Verification
|
PROTACs
CDK
|
Cancer
|
CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6 .
|
-
- HY-143713
-
|
Aurora Kinase
|
Cancer
|
Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A. Aurora A has been implicated in cancers of diverse histological origin and may possess oncogenic properties when overexpressed. Aurora A inhibitor 1 has the potential for the research of cancer diseases mediated by aurora a (extracted from patent WO2021147974A1, compound 49) .
|
-
- HY-144671
-
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-144669
-
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-P99233
-
HuMax-TAC
|
Interleukin Related
|
Cancer
|
Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
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-
- HY-157484
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
|
-
- HY-121364
-
|
Histamine Receptor
Fluorescent Dye
|
Others
|
Bodilisant is a fluorescent histamine H3 receptor ligand. Bodilisant can be used at low concentrations (1-10 nM) to detect the performance of hH3R in cells overexpressing hH3R, and at about 1 μM concentration for tissues rich in hH3R. Bodilisant is a useful pharmacological tool for receptor imaging .
|
-
- HY-118386
-
|
Others
|
Metabolic Disease
|
H2-005 is a compound that selectively inhibits diacylglycerol acyltransferase 2 (DGAT2) and has the activity to inhibit triacylglycerol synthesis in hepatocytes and preadipocytes. H2-005 significantly reduces triacylglycerol biosynthesis in HepG2 hepatocytes and 3T3-L1 preadipocytes. H2-005 exhibits specific inhibitory activity in DGAT2-overexpressing HEK293 cells. H2-005 almost completely inhibits lipid droplet formation in 3T3-L1 cells when co-treated with a DGAT1 inhibitor. H2-005 will contribute to DGAT2-related lipid metabolism research and the development of drugs to inhibit metabolic diseases .
|
-
- HY-129390
-
ICP-022
|
Btk
|
Cancer
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK .
|
-
- HY-123781A
-
|
Hedgehog
|
Cancer
|
RUSKI-201 dihydrochloride is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 0.20 μM. RUSKI-201 dihydrochloride is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 dihydrochloride is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function .
|
-
- HY-145898
-
14-D-Valine-TPL
|
c-Myc
Molecular Glues
|
Cancer
|
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
|
-
- HY-161456
-
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
PHGDH-IN-5 (Compound B12) is a covalen inhibitor of PHGDH with an IC50 value of 0.29 μM. PHGDH-IN-5 can inhibit cell proliferation in cancer cell lines overexpressing PHGDH. PHGDH-IN-5 can reduce the production of serine derived from glucose in MDA-MB-468 cells .
|
-
- HY-123781
-
|
Hedgehog
|
Cancer
|
RUSKI-201 is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor, with an IC50 of 0.20 μM. RUSKI-201 is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function .
|
-
- HY-106265
-
|
P-glycoprotein
|
Cancer
|
9,10-trans-Dehydroepothilone D shows an antiproliferative activity against a paclitaxel-resistant cell lines overexpressing P-glycoprotein. 9,10-trans-Dehydroepothilone D also shows tubulin polymerization activity. 9,10-trans-Dehydroepothilone D is given by lactonization of Seco acid, which is promising for research of cancers .
|
-
- HY-155035
-
|
Others
|
Cancer
|
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .
|
-
- HY-P99161
-
BGB149
|
TAM Receptor
|
Cancer
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
|
-
- HY-153396
-
|
Ceramidase
|
Cancer
|
Acid Ceramidase-IN-2 (compound 1) is an acid ceramidase inhibitor with potentially antiproliferative and cytostatic activities. Moreover, human acid ceramidase is overexpressed in prostate cancer cells, indicating potential anti-tumor effect of Acid Ceramidase-IN-2. And Acid Ceramidase-IN-2 hydrolysis can be inhibited by 3 a-ketoamides GT85, GT98 and GT99 inhibits in vitro .
|
-
- HY-163146
-
|
Fluorescent Dye
|
Cancer
|
TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
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-
- HY-119234
-
|
Others
|
Inflammation/Immunology
|
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
|
-
- HY-114358
-
ONO-7475
|
TAM Receptor
Trk Receptor
|
Cancer
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
|
-
- HY-111083
-
CID23612552
|
GPR55
|
Others
|
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .
|
-
- HY-159009
-
|
NAMPT
|
Cancer
|
MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). NAMPT is the rate-limiting enzyme in the NAD + biosynthetic pathway, responsible for converting nicotinamide to nicotinamide mononucleotide, which is then converted to NAD +. NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD + required for rapid proliferation. PROTAC A7, a derivative of MS7, is an effective NAMPT degrader. MS7 can be used in cancer research .
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-
- HY-120432
-
|
Others
|
Infection
|
CaMdr1p-IN-1 (Compound A) is an inhibitor for the major facilitator superfamily transporter CaMdr1p. CaMdr1p-IN-1 exhibits chemosensitizing efficacy. CaMdr1p-IN-1 synergizes with Fluconazole (HY-B0101), that inhibits CaMdr1p overexpressing Candida albicans with MIC of 10 μM .
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-
- HY-164537
-
|
Phosphatase
MDM-2/p53
Apoptosis
|
Cancer
|
SPI-001 is a PPM1D-specific inhibitor (IC50=0.48 μM) with anticancer activity. SPI-001 inhibits PPM1D phosphatase activity and increases p53 phosphorylation in PPM1D-overexpressing human breast cancer cells. In addition, SPI-001 inhibits cell proliferation by inducing apoptosis .
|
-
- HY-N2416
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities . Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis . Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells .
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-
- HY-P10524
-
|
Nectin-4
|
Cancer
|
N188 is a radioligand based on a bicyclic peptide backbone that targets nectin-4, a protein overexpressed in many tumors. N188 can be efficiently radiolabeled to 68Ga-N188, a radioisotope suitable for positron emission tomography (PET) imaging. The development of N188 and its radiolabeled form 68Ga-N188 can be used for the diagnosis and treatment of tumors such as urothelial carcinoma .
|
-
- HY-103441
-
|
EGFR
|
Cancer
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
|
-
- HY-P99506
-
SC-003 mAb; SC-Mab003; SC34.28ss1
|
ADC Antibody
|
Cancer
|
Tamrintamab (SC-003 mAb, SC-Mab003, SC34.28ss1) is an ADC Antibody targeting to dipeptidase 3 (DPEP3 or MBD3). DPEP3 is a glycosyl phosphatidylinositol anchored metallopeptidase that is overexpressed in ovarian tumors. Tamrintamab can specifically bind DPEP3-expressing cells to produce cytotoxicity. Tamrintamab can be used in ovarian cancer research .
|
-
- HY-155659
-
|
Nuclear Hormone Receptor 4A/NR4A
|
Neurological Disease
|
4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease .
|
-
- HY-162567
-
|
HSP
|
Cancer
|
AP-4-139B is a heat shock protein 70 inhibitor (IC50=180 nM). HSP70 is a protein that is overexpressed in many types of cancer and is closely related to the survival and proliferation of tumor cells. AP-4-139B exhibits significant cytotoxicity to tumor cells, particularly in colorectal cancer cells. AP-4-139B can be used for cancer research .
|
-
- HY-169083
-
|
Apoptosis
Bcl-2 Family
|
Cancer
|
Bcl-2-IN-22 (compound 1) is a gold(I) NHC complex with anticancer activity. Bcl-2-IN-22 induces apoptosis via the mitochondrial pathway with an IC50 value of 0.014 μM. In addition, Bcl-2-IN-22 targets BCL-2 family members and exhibits pro-apoptosis and resensitization properties in multidrug-resistant leukemia cells that overexpress BCL?2 .
|
-
- HY-136057
-
|
Ferroptosis
|
Cancer
|
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A) .
|
-
- HY-P10524A
-
|
Nectin-4
|
Cancer
|
N188 TFA is a radioligand based on a bicyclic peptide backbone that targets nectin-4, a protein overexpressed in many tumors. N188 TFA can be efficiently radiolabeled to 68Ga-N188, a radioisotope suitable for positron emission tomography (PET) imaging. The development of N188 TFA and its radiolabeled form 68Ga-N188 can be used for the diagnosis and treatment of tumors such as urothelial carcinoma .
|
-
- HY-129636A
-
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-N10264
-
(+)-Avrainvillamide; CJ-17,665
|
Antibiotic
|
Infection
Cancer
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
- HY-144749
-
|
Others
|
Cancer
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-156088
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
|
-
- HY-129284
-
|
COX
|
Cancer
|
APHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition .
|
-
- HY-118013
-
|
Others
|
Infection
|
NDM-1 inhibitor-2 is an inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) and has the ability to inhibit NDM-1 activity. NDM-1 inhibitor-2 exhibits a good inhibitory effect on drug-resistant bacterial strains that overexpress NDM-1. When NDM-1 inhibitor-2 is used in combination with the carbapenem antibiotic meropenem, a favorable synergistic effect can be produced .
|
-
- HY-164474
-
|
MEK
|
Cancer
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-155760
-
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
|
-
- HY-129636
-
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-110333
-
|
EGFR
|
Cancer
|
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
|
-
- HY-B0530A
-
γ-pipradol hydrochloride
|
Others
|
Cancer
|
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
|
-
- HY-147826
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
- HY-P5520
-
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-118899
-
|
Others
|
Cancer
|
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
|
-
- HY-117051
-
|
Others
|
Cancer
|
STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
|
-
Cat. No. |
Product Name |
Type |
-
- HY-149835
-
|
Fluorescent Dyes/Probes
|
TTX-P is a fluorescent probe. TTX-P responds in situ to the overexpressed alkaline phosphatase (ALP) in liver, imaging of diabetic liver injury in the near-infrared second-window (NIR-II) region .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2508
-
|
Mucin
|
Cancer
|
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .
|
-
- HY-107760A
-
-
- HY-P2526A
-
|
Peptides
|
Cancer
|
LyP-1 TFA is a cyclic 9 amino acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
|
-
- HY-136626
-
Cbz-Ala-Ala-Asn-AMC
|
Fluorescent Dye
|
Cancer
|
Z-Ala-Ala-Asn-AMC (Cbz-Ala-Ala-Asn-AMC) is the legumain substrate. Overexpressed legumain in 293 HEK-Leg cells potently cleaved CBZ-Ala-Ala-Asn-AMC .
|
-
- HY-P10328
-
|
DNA/RNA Synthesis
|
Metabolic Disease
|
Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
|
-
- HY-P2526
-
|
Peptides
|
Cancer
|
LyP-1 is a cyclic 9‐amino‐acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
|
-
- HY-P10561
-
|
Peptides
|
Cancer
|
CPK peptide is a tumor-localizing peptide. CPK peptide specifically binds to the monocarboxylate transporter 1 (MCT1) receptor, which is overexpressed in many human colon cancer cell lines but not in normal cells. CPK peptide can be used in tumor diagnosis research .
|
-
- HY-P10524
-
|
Nectin-4
|
Cancer
|
N188 is a radioligand based on a bicyclic peptide backbone that targets nectin-4, a protein overexpressed in many tumors. N188 can be efficiently radiolabeled to 68Ga-N188, a radioisotope suitable for positron emission tomography (PET) imaging. The development of N188 and its radiolabeled form 68Ga-N188 can be used for the diagnosis and treatment of tumors such as urothelial carcinoma .
|
-
- HY-P2524
-
|
Peptides
|
Cancer
|
MAGE-3 (271-279) is a 271-279 residue peptide derived from melanoma antigens encoded by MAGE-3. MAGE-3 is a cytolytic T lymphocyte (CTL)-defined MAGE-3 protein associated with the human leukocyte antigen (HLA)-A2 molecule. MAGE-3 is overexpressed in different human tumor types, including malignant melanoma, but not by normal tissues except for testis and placenta .
|
-
- HY-P5472
-
|
Peptides
|
Others
|
Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
|
-
- HY-P10524A
-
|
Nectin-4
|
Cancer
|
N188 TFA is a radioligand based on a bicyclic peptide backbone that targets nectin-4, a protein overexpressed in many tumors. N188 TFA can be efficiently radiolabeled to 68Ga-N188, a radioisotope suitable for positron emission tomography (PET) imaging. The development of N188 TFA and its radiolabeled form 68Ga-N188 can be used for the diagnosis and treatment of tumors such as urothelial carcinoma .
|
-
- HY-P1137
-
|
Peptides
|
Others
|
10Panx is a biological active peptide. (This is a Pannexin-1 (Panx1) mimetic blocking peptide. Pannexin-1 is a recently identified membrane protein that can form gap junction-like connections allowing intercellular passage of dyes when overexpressed in two adjacent oocytes or mammalian epithelial cell lines. Blockade of pannexin-1 in macrophage endogenously expressing the ATP-gated P2X7 receptor (P2X7R) blocks the initial dye uptake, but not the ionic current, and also blocks processing and release of interleukin-1b (IL-1b) in response to P2X7R activation.)
|
-
- HY-P5520
-
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99700
-
IBI-188
|
Inhibitory Antibodies
|
Cancer
|
Letaplimab (IBI-188) is a human IgG4 anti-CD47 monoclonal antibody. CD47 is overexpressed on cancer cells, it is a ligand for SIRPα. Letaplimab enhances tumor cell phagocytosis .
|
-
- HY-P9907
-
Anti-Human HER2, Humanized Antibody
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
ADC Antibody
|
Cancer
|
Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
- HY-P9907A
-
Anti-Human HER2, Humanized Antibody (PBS)
|
ADC Antibody
EGFR
|
Cancer
|
Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
- HY-P99153
-
MORAb-003
|
Antibiotic
|
Cancer
|
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
|
-
- HY-P99566
-
ST2146
|
Inhibitory Antibodies
|
Cancer
|
Tenatumomab (ST2146) is a murine monoclonal antibody against tenascin-C. And tenascin-C, the large extracellular glycoprotein, is overexpressed in cancer. Tenatumomab has been used for Pretargeted Antibody Guided Radioimmunoresearch (PAGRIT), and delivering radionuclides to tumors via PAGRIT and direct 131Iodine labeling approach .
|
-
- HY-P99233
-
HuMax-TAC
|
Interleukin Related
|
Cancer
|
Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
|
-
- HY-P99161
-
BGB149
|
TAM Receptor
|
Cancer
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
|
-
- HY-P99506
-
SC-003 mAb; SC-Mab003; SC34.28ss1
|
ADC Antibody
|
Cancer
|
Tamrintamab (SC-003 mAb, SC-Mab003, SC34.28ss1) is an ADC Antibody targeting to dipeptidase 3 (DPEP3 or MBD3). DPEP3 is a glycosyl phosphatidylinositol anchored metallopeptidase that is overexpressed in ovarian tumors. Tamrintamab can specifically bind DPEP3-expressing cells to produce cytotoxicity. Tamrintamab can be used in ovarian cancer research .
|
-
- HY-P99630
-
MM-302
|
EGFR
|
Cancer
|
Gancotamab (MM-302) is a HER2-targeted antibody-liposomal Doxorubicin conjugate with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells .
|
-
- HY-P99516
-
HLX-06
|
VEGFR
|
Cancer
|
Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2103
-
-
-
- HY-P9907
-
-
-
- HY-P9907A
-
-
-
- HY-P99153
-
-
-
- HY-N3028
-
-
-
- HY-P99161
-
BGB149
|
Classification of Application Fields
Disease Research Fields
Cancer
|
TAM Receptor
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
|
-
-
- HY-N2416
-
-
-
- HY-N10264
-
(+)-Avrainvillamide; CJ-17,665
|
Infection
Alkaloids
Structural Classification
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Source classification
Disease Research Fields
Indole Alkaloids
|
Antibiotic
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
-
- HY-P99630
-
-
-
- HY-N144114
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-135336S
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(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
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Cat. No. |
Product Name |
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Classification |
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- HY-10822A
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BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
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Alkynes
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ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
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- HY-10822
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BGC 945; ONX-0801
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Alkynes
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Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
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Cat. No. |
Product Name |
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Classification |
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- HY-142118A
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AP 12009 sodium
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Antisense Oligonucleotides
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Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
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- HY-158828
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Antisense Oligonucleotides
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SSO111 sodium, a 20mer fully modified antisense oligonucleotide, targets the oncogene?HER2. SSO111 sodium induces exon 15 skipping during splicing, leading to the generation of a novel mRNA transcript that excludes exon 15. SSO111 sodium downregulated HER2 mRNA, which resulted in the inhibition of proliferation and induction of apoptosis in HER2-overexpressing tumor cells.
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- HY-160050
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Aptamers
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CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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- HY-160051
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Aptamers
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CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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- HY-142118
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AP 12009
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Antisense Oligonucleotides
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Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
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