Search Result
Results for "
overexpress
" in MedChemExpress (MCE) Product Catalog:
12
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101280
-
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NAMPT
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Cancer
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LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
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- HY-P2508
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Mucin
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Cancer
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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 .
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- HY-162470
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Aurora Kinase
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Cancer
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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 .
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- HY-100111
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GLX351322
Maximum Cited Publications
37 Publications Verification
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NADPH Oxidase
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Metabolic Disease
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GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μM.
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- HY-164136
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17β-HSD
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Metabolic Disease
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17β-HSD5 inhibitor 1 (Compound 29) is a potent 17β-HSD5 inhibitor, with an IC50 of 2.9 nM in HEK-293 cells overexpressing human 17β-HSD5 .
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- HY-101280A
-
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NAMPT
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Cancer
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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 .
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- HY-163919
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Topoisomerase
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Cancer
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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 .
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- HY-149389
-
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Adrenergic Receptor
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Endocrinology
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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 .
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- HY-P99630
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MM-302
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EGFR
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Cancer
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Gancotamab (MM-302) is a HER2-targeted antibody with antitumor activity. Gancotamab encapsulates Doxorubicin to facilitate its delivery to HER2-overexpressing tumor cells .
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- HY-P10328
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DNA/RNA Synthesis
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Metabolic Disease
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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.
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- HY-156244
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PROTACs
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Cancer
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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 .
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- HY-135336S
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(R)-(+)-Verapamil-d7 hydrochloride
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P-glycoprotein
Isotope-Labeled Compounds
Apoptosis
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Cancer
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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 .
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- HY-W702292
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Isotope-Labeled Compounds
Apoptosis
P-glycoprotein
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Cancer
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(R)-(+)-Verapamil-d6 (hydrochloride) is 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 .
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- HY-163918
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P-glycoprotein
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Cancer
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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 .
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- HY-156418
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DNA/RNA Synthesis
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Cancer
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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 .
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- HY-156243
-
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ROCK
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Cancer
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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 .
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- HY-107760
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- HY-169244
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CDK
Bcl-2 Family
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Cancer
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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 .
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- HY-107760A
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- HY-169240
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MDM-2/p53
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Cancer
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MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .
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- HY-P11078A
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EGFR
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Cancer
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LARLLT TFA is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer .
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- HY-158828
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EGFR
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Cancer
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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-P11078
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EGFR
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Cancer
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LARLLT (D4) is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer .
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- HY-10822A
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BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
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Thymidylate Synthase
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Cancer
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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-100416
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GlyT
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Neurological Disease
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LY2365109 is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a .
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- HY-100416A
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GlyT
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Neurological Disease
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LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a .
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- HY-50883
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γ-secretase
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Neurological Disease
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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).
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- HY-157942
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Cytochrome P450
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Cancer
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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) .
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- HY-P2526
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LyP-1
2 Publications Verification
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Complement System
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Cancer
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LyP-1 is a cyclic 9-amino-acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
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- HY-132934
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BCRP
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Cancer
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Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in the
BCRP-overexpressed HEK293/R2 cells.
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- HY-115831
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S1P1 agonist 3
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LPL Receptor
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Cardiovascular Disease
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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 .
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- HY-N2103
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P-glycoprotein
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Cancer
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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 .
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- HY-100395
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Apoptosis
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Cancer
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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.
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- HY-153889
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- HY-10822
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BGC 945; ONX-0801
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Thymidylate Synthase
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Others
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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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- HY-149835
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Fluorescent Dye
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Others
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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 .
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- HY-136626
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Cbz-Ala-Ala-Asn-AMC
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Fluorescent Dye
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Cancer
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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 .
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- HY-16191
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Microtubule/Tubulin
Apoptosis
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Cancer
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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.
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- HY-158025
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DNA/RNA Synthesis
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Cancer
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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 .
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- HY-33299
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BTCA
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Biochemical Assay Reagents
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Cancer
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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) .
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- HY-P9907A
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Anti-Human HER2, Humanized Antibody (PBS)
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ADC Antibody
EGFR
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Cancer
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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.
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- HY-157483
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P-glycoprotein
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Cancer
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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 .
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- HY-147637
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Ephrin Receptor
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Cancer
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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 .
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- HY-P99516
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HLX-06
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VEGFR
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Cancer
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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 .
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- HY-W012670
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Apoptosis
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Cancer
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2-Deoxy-L-ribose is a stereoisomer of 2-Deoxy-d-ribose that inhibits 2-Deoxy-d-ribose anti-apoptotic effects. 2-Deoxy-L-ribose suppresses metastasis of tumor cells overexpressing thymidine phosphorylase .
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- HY-173405
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Ras
PI3K
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Cancer
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VVD-699 is a covalent RAS-PI3K inhibitor. VVD-699 covalently binds to cysteine 242 in the RAS binding domain of PI3K p110α, thereby blocking the ability of RAS to activate PI3K activity. VVD-699 is able to inhibit the growth of RAS-mutated and HER2-overexpressing tumors. VVD-699 can be used to study cancers associated with RAS mutations (e.g., H358 lung cancer cells, A549 cells, FaDu cells) .
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- HY-146393
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PROTACs
Cytochrome P450
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Cancer
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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 .
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- HY-155763
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VEGFR
Carbonic Anhydrase
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Cancer
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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 .
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- HY-155758
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VEGFR
Carbonic Anhydrase
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Cancer
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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 .
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- HY-114877
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Phosphatase
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Cancer
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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 .
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- HY-P99153
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MORAb-003
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Antibiotic
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Cancer
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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 .
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- HY-N144114
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P-glycoprotein
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Cancer
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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) .
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- HY-142118A
-
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AP 12009 sodium
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TGF-beta/Smad
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Cancer
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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-169868
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Biochemical Assay Reagents
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Cancer
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NOTA-FAPI-52 is a tracer with potent tumor uptake. NOTA-FAPI-52 can be radiolabeled to enable PET imaging or other bioimaging techniques. NOTA-FAPI-52 can be used to study diseases in which fibroblast activation protein (FAP) is overexpressed .
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- HY-109050
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GS-5829
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-172272B
-
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Liposome
VEGFR
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Cancer
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DSPE-PEG5000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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- HY-172272A
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Liposome
VEGFR
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Cancer
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DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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- HY-172272
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Liposome
VEGFR
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Cancer
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DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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- HY-172272C
-
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Liposome
VEGFR
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Cancer
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DSPE-PEG3400-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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- HY-12762
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QS11
1 Publications Verification
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β-catenin
Wnt
Arf Family GTPase
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Cancer
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QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
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- HY-138084
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Separase
Mitosis
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Cancer
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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 .
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- HY-P99566
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ST2146
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Transmembrane Glycoprotein
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Cancer
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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 .
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- HY-142118
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AP 12009
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TGF-beta/Smad
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Cancer
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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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- HY-172471
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Liposome
EGFR
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Cancer
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DSPE-PEG5000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG5000-GE11 can be used for drug delivery .
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- HY-172470A
-
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Liposome
EGFR
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Cancer
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DSPE-PEG3400-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG3400-GE11 can be used for drug delivery .
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- HY-162318
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Molecular Glues
c-Myc
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Cancer
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MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
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- HY-172275A
-
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Liposome
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Inflammation/Immunology
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DSPE-PEG2000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG2000-pPB can be used for drug delivery .
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- HY-172470
-
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Liposome
EGFR
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Cancer
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DSPE-PEG2000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG2000-GE11 can be used for drug delivery .
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- HY-125835
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CP-10
1 Publications Verification
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PROTACs
CDK
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Cancer
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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 .
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- HY-172275
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Liposome
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Inflammation/Immunology
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DSPE-PEG1000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG1000-pPB can be used for drug delivery .
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- HY-172469
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Liposome
EGFR
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Cancer
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DSPE-PEG1000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG1000-GE11 can be used for drug delivery .
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- HY-N3028
-
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-172275B
-
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Liposome
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Inflammation/Immunology
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DSPE-PEG5000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG5000-pPB can be used for drug delivery .
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- HY-172275C
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Liposome
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Inflammation/Immunology
|
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DSPE-PEG3400-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG3400-pPB can be used for drug delivery .
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-
- HY-101997
-
|
|
Apoptosis
Caspase
|
Infection
Cancer
|
|
BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) inducer and antiviral agent. BEPP hydrochloride effectively inhibits the growth of human lung cancer cell lines overexpressing PKR and induces apoptosis and activates caspase-3 in sensitive cells. In addition, BEPP hydrochloride can also significantly inhibit vaccinia virus replication .
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-
- 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 .
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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 .
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-
- HY-162318A
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
|
-
- 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) .
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-
- 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 .
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-
- 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 .
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-
- HY-118386
-
|
|
Endogenous Metabolite
|
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 .
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-
- 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-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 .
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-
- 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 .
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-
- HY-159009
-
|
|
NAMPT
Ligands for Target Protein for PROTAC
|
Cancer
|
|
MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD + required for rapid proliferation. MS7, as a NAMPT target protein ligand, can be used to synthesize PROTAC A7, which is an effective NAMPT degrader. MS7 can be used in cancer research .
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-
- 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 .
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-
- 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-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 .
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-
- 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-155035
-
|
|
17β-HSD
|
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 .
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-
- 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 .
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-
- HY-119234
-
|
|
CXCR
|
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 .
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-
- HY-120432
-
|
|
Fungal
ATP-binding cassette (ABC) transporters
|
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-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 .
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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 .
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-
- 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).
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-
- 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-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 .
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-
- 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 .
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-
- 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 .
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-
- HY-P5472
-
|
|
Transmembrane Glycoprotein
|
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.)
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-
- 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 .
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-
- 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-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) .
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-
- HY-P2671
-
|
|
Cholecystokinin Receptor
|
Cancer
|
|
[Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
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-
![[Leu15]-Gastrin I (human)](//file.medchemexpress.eu/product_pic/hy-p2671.gif)
- HY-156088
-
|
|
Apoptosis
Microtubule/Tubulin
Mitosis
|
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-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 .
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-
- HY-129284
-
|
|
COX
Wnt
|
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-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-118013
-
|
|
Bacterial
|
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 .
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-
- HY-144749
-
|
|
Aldose Reductase
|
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-156513
-
|
7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)
|
ADC Cytotoxin
|
Cancer
|
|
ZD06519 (7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)) is a camptothecin (HY-16560) analogue and a topoisomerase I inhibitor. ZD06519 is an ADC cytotoxin with a strong bystander effect, inhibiting a variety of malignancies such as HER2-positive and FRα-overexpressing tumors. ZD06519 inhibits DNA cleavage, relaxation, and reconnection processes, inducing tumor cell death. ZD06519 can be used for ADC synthesis and cancer research .
|
-
- 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-168953
-
|
|
P-glycoprotein
Apoptosis
Bcl-2 Family
Reactive Oxygen Species (ROS)
Caspase
|
Cancer
|
|
Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
|
-
- HY-147007
-
|
|
β-catenin
Wnt
CDK
|
Cancer
|
|
β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells .
|
-
- HY-176019
-
|
|
p38 MAPK
c-Myc
|
Cardiovascular Disease
Cancer
|
|
Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy .
|
-
- 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
|
Reactive Oxygen Species (ROS)
mAChR
NADPH Oxidase
|
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-P99682
-
|
hLIV22
|
ADC Antibody
|
Cancer
|
|
Ladiratuzumab (hLIV22) is a humanized monoclonal antibody against zinc transporter LIV-1/ZIP6. Ladiratuzumab is conjugated to MMAE (HY-15162) via a cleavable dipeptide linker to synthesize an antibody-drug conjugate (ADC) Ladiratuzumab vedotin (HY-P99683). Ladiratuzumab vedotin selectively targets LIV-1 protein overexpressed on the surface of tumor cells, enters cells through antibody-mediated receptor endocytosis, releases MMAE to inhibit microtubule polymerization, and kills adjacent tumor cells with a bystander effect. Ladiratuzumab can be used in the study of solid tumors such as metastatic triple-negative breast cancer (mTNBC) .
|
-
- 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-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-118899
-
|
|
Endogenous Metabolite
|
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-138089
-
|
|
Androgen Receptor
Estrogen Receptor/ERR
LDLR
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Metabolic Disease
Cancer
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17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
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| Cat. No. |
Product Name |
Type |
-
- HY-149835
-
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Fluorescent Dyes/Probes
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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 .
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| Cat. No. |
Product Name |
Type |
-
- HY-172275A
-
|
|
Drug Delivery
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DSPE-PEG2000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG2000-pPB can be used for drug delivery .
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-
- HY-W012670
-
|
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Carbohydrates
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2-Deoxy-L-ribose is a stereoisomer of 2-Deoxy-d-ribose that inhibits 2-Deoxy-d-ribose anti-apoptotic effects. 2-Deoxy-L-ribose suppresses metastasis of tumor cells overexpressing thymidine phosphorylase .
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-
- HY-172272B
-
|
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Drug Delivery
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DSPE-PEG5000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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-
- HY-172272A
-
|
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Drug Delivery
|
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DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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- HY-172272
-
|
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Drug Delivery
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DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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-
- HY-172272C
-
|
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Drug Delivery
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DSPE-PEG3400-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
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-
- HY-172470A
-
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Drug Delivery
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DSPE-PEG3400-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG3400-GE11 can be used for drug delivery .
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-
- HY-172470
-
|
|
Drug Delivery
|
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DSPE-PEG2000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG2000-GE11 can be used for drug delivery .
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-
- HY-172275
-
|
|
Drug Delivery
|
|
DSPE-PEG1000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG1000-pPB can be used for drug delivery .
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-
- HY-172469
-
|
|
Drug Delivery
|
|
DSPE-PEG1000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG1000-GE11 can be used for drug delivery .
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-
- HY-172275B
-
|
|
Drug Delivery
|
|
DSPE-PEG5000-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG5000-pPB can be used for drug delivery .
|
-
- HY-172275C
-
|
|
Drug Delivery
|
|
DSPE-PEG3400-pPB is a PEG compound which composed of DSPE and a cyclic oligopeptide (pPB). pPB has a strong binding affinity with PDGFRβ, which is overexpressed on activated hepatic stellate cells (HSC). DSPE-PEG3400-pPB can be used for drug delivery .
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| 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-P2526
-
LyP-1
2 Publications Verification
|
Complement System
|
Cancer
|
|
LyP-1 is a cyclic 9-amino-acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
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-
- 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 .
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-
- 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 .
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-
- 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-P11078A
-
|
|
EGFR
|
Cancer
|
|
LARLLT TFA is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer .
|
-
- HY-P11078
-
|
|
EGFR
|
Cancer
|
|
LARLLT (D4) is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer .
|
-
- 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 .
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-
- 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
-
|
|
Transmembrane Glycoprotein
|
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.)
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-
- HY-P2671
-
|
|
Cholecystokinin Receptor
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Cancer
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|
[Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
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-
- 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 .
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-
- 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
|
Transmembrane Glycoprotein
|
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-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-P99682
-
|
hLIV22
|
ADC Antibody
|
Cancer
|
|
Ladiratuzumab (hLIV22) is a humanized monoclonal antibody against zinc transporter LIV-1/ZIP6. Ladiratuzumab is conjugated to MMAE (HY-15162) via a cleavable dipeptide linker to synthesize an antibody-drug conjugate (ADC) Ladiratuzumab vedotin (HY-P99683). Ladiratuzumab vedotin selectively targets LIV-1 protein overexpressed on the surface of tumor cells, enters cells through antibody-mediated receptor endocytosis, releases MMAE to inhibit microtubule polymerization, and kills adjacent tumor cells with a bystander effect. Ladiratuzumab can be used in the study of solid tumors such as metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-P99630
-
|
MM-302
|
EGFR
|
Cancer
|
|
Gancotamab (MM-302) is a HER2-targeted antibody 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-N3028
-
-
-
- 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-N144114
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-135336S
-
|
|
|
(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 .
|
-
-
- HY-W702292
-
|
|
|
(R)-(+)-Verapamil-d6 (hydrochloride) is 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 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-10822A
-
|
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
|
Alkynes
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
|
-
- HY-10822
-
|
BGC 945; ONX-0801
|
|
Alkynes
|
|
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 .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-142118A
-
|
AP 12009 sodium
|
|
Antisense Oligonucleotides
|
|
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-142118
-
|
AP 12009
|
|
Antisense Oligonucleotides
|
|
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-158828
-
|
|
|
Antisense Oligonucleotides
|
|
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-160050
-
|
|
|
Aptamers
|
|
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 .
|
-
- HY-160051
-
|
|
|
Aptamers
|
|
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 .
|
-
- HY-172470
-
|
|
|
Pegylated Lipids
|
|
DSPE-PEG2000-GE11 is a PEG compound which composed of DSPE and an EGFR targeting peptide (GE11). GE11 can be used for EGFR overexpressed cancer cells. DSPE-PEG2000-GE11 can be used for drug delivery .
|
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