Ephrin Receptor Inhibitor

ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC₅₀ of 11 nM for Eph2.

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.

ALW-II-49-7 is a selective EphB2 kinase inhibitor with an EC₅₀ value of 40 nM in cell.

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.

EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC₅₀ values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.

MBRC-101 Antibody is a human monoclonal antibody targeting EphA5. MBRC-101 Antibody can be used to synthesize the ADC MBRC-101.

Anti-EphB3 Antibody is an anti-EphB3 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

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.

Anti-EphA2 Antibody (1C1) (MEDI-547 antibody) is an anti-EphA2 monoclonal antibody. Anti-EphA2 Antibody (1C1) can induce degradation of EphA2 protein. Anti-EphA2 Antibody (1C1) conjugated with McMMAF (HY-15578) can form an antibody-conjugated drugs, which has potent antitumor activity. Anti-EphA2 Antibody (1C1) can be used for the research of cancer, such as prostate cancer and glioma.

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.

JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.

Eph inhibitor 1 is a potent Eph inhibitor. Eph inhibitor 1 has the potential for the research of neurological disorders.

EphA2 antagonist 1 (4b) is a bile acid conjugate and an ephrin type-A receptor 2 (EPHA2) inhibitor.

UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis.

A11 (ANXA1-derived 11 amino acid-long peptide) is a ANXA1-EphA2 interaction-blocking peptide. A11 reduces ANXA1 bound to EphA2 and increases Cbl (the E3 ubiquitin ligase of EphA2) bound to EphA2. A11 inhibits the proliferation, migration and invasion of nasopharyngeal carcinoma cells. A11 inhibits angiogenesis. A11 can be used in studies related to nasopharyngeal carcinoma.

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.

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 K_i 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.

The Anti-EphB2 Antibody is a CHO expressed human antibody that targets EphB2. The Anti-EphB2 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-EphB2 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

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.

DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with ⁸⁹Zr, ¹¹¹In, or ¹²⁵I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo..