2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Ephrin Receptor
  5. Ephrin Receptor Inhibitor

Ephrin Receptor Inhibitor

Ephrin Receptor Isoform Comparison

Ephrin Receptor Inhibitors (27):

Cat. No. Product Name Effect Purity
  • HY-13258A
    NVP-BHG712
    		Inhibitor 99.71%
    NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively.
  • HY-18007
    ALW-II-41-27
    		Inhibitor 99.38%
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
  • HY-18833
    ALW-II-49-7
    		Inhibitor 99.97%
    ALW-II-49-7 is a selective EphB2 kinase inhibitor with an EC50 value of 40 nM in cell.
  • HY-18832
    AWL-II-38.3
    		Inhibitor 99.71%
    AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf.
  • HY-P991577
    DS-8895
    		Inhibitor
    DS-8895 is an anti-EphA2 monoclonal antibody. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. DS-8895 can be studied in research for advanced solid cancers positive to EphA2.
  • HY-P10412A
    A11 acetate
    		Inhibitor
    A11 (ANXA1-derived 11 amino acid-long peptide) acetate is an ANXA1-EphA2 interaction blocker peptide. A11 acetate decreases ANXA1 bound to EphA2 and increased Cbl (an E3 ubiquitin ligase of EphA2) bound to EphA2. A11 efficiently decreases EphA2 level, and substantially increases EphA2 ubiquitination. A11 acetate increases EphA2 internalization and colocalization of EphA2 and Cbl in the NPC cells. A11 acetate inhibits nasopharyngeal carcinoma (NPC) cell proliferation, migration and invasion. A11 acetate inhibits angiogenesis.
  • HY-107460
    LDN-211904 oxalate
    		Inhibitor ≥99.0%
    LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC.
  • HY-16265
    JI-101
    		Inhibitor 99.78%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
  • HY-P2264
    KYL peptide
    		Inhibitor 99.09%
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-114199
    Eph inhibitor 1
    		Inhibitor 99.92%
    Eph inhibitor 1 is a potent Eph inhibitor. Eph inhibitor 1 has the potential for the research of neurological disorders.
  • HY-17617
    Nastorazepide
    		Inhibitor 99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
  • HY-170517
    PKMYT1-IN-8
    		Inhibitor 99.31%
    PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC50 of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC50s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI50 of 2.02 μM.
  • HY-169849
    EphA2 antagonist 1
    		Inhibitor
    EphA2 antagonist 1 (4b) is a bile acid conjugate and an ephrin type-A receptor 2 (EPHA2) inhibitor.
  • HY-148065
    FMF-06-098-1
    		Inhibitor 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 (Pink: target protein ligand (HY-169396); Blue: VHL ligand (HY-112078); Black: Linker (HY-124380)).
  • HY-P10412
    A11
    		Inhibitor
    A11 (ANXA1-derived 11 amino acid–long peptide) is an ANXA1-EphA2 interaction blocker peptide. A11 decreases ANXA1 bound to EphA2 and increased Cbl (an E3 ubiquitin ligase of EphA2) bound to EphA2. A11 efficiently decreases EphA2 level, and substantially increases EphA2 ubiquitination. A11 increases EphA2 internalization and colocalization of EphA2 and Cbl in the NPC cells. A11 inhibits nasopharyngeal carcinoma (NPC) cell proliferation, migration and invasion. A11 inhibits angiogenesis.
  • HY-155685
    SA-VA
    		Inhibitor
    SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase.
  • HY-159174
    EPHA2/A4/GAK-IN-1
    		Inhibitor
    EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells.
  • HY-161171
    Antimalarial agent 37
    		Inhibitor
    Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7.
  • HY-14575
    Nastorazepide hemicalcium
    		Inhibitor
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
  • HY-14979A
    ML786 dihydrochloride
    		Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.