Cancer Targeted Therapy

HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC₅₀=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.

Praluzatamab is a monoclonal antibody targeting the activated leukocyte cell adhesion molecule (ALCAM/CD116). Praluzatamab can be used to synthesize Praluzatamab ravtansine (antibody-drug conjugates). Praluzatamab can be used for research of cancers.

Cosibelimab (CK-301) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab exhibits antitumor efficacy.

Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a K_D of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology.

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC₅₀ of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC₅₀=80 nM).

CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC₅₀s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells.

CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.

MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.

TAS1553 is a potent, orally active protein-protein interaction (PPI) inhibitor with an IC₅₀ values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.

TL13-112 is a ALK PROTAC degrader. TL13-112 degrades the NPM-ALK protein by recruiting the CRBN E3 ligase, thereby blocking oncogenic signal transduction such as STAT3, ERK and AKT, and relieving the transcriptional repression of CD45, CCR7 and PI3Kδ. TL13-112 can be used in related research on anaplastic large cell lymphoma.

Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs.

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

GNQWFI, an anti-Flt1 peptide, is a VEGFR1-specific antagonist. GNQWFI blocks the interaction of VEGFR1 with various VEGFR1 ligands, such as VEGFA, VEGFB, and placental growth factor (PIGF) and inhibits VEGF-induced endothelial cell migration and tube formation. GNQWFI is promising for research of cancer, asthma, and other ocular diseases.

VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer.

DSPE-PEG2000-TCO is a click chemistry coupling partner. DSPE-PEG2000-TCO undergoes a reverse electron-demand Diels-Alder click reaction to form a covalent linkage with tetrazine-modified Cetuximab (HY-P9905). DSPE-PEG2000-TCO maintains the stability of lipid nanoparticles (LNPs) and has high mRNA encapsulation efficiency, which supports cellular uptake and mRNA transfection. DSPE-PEG2000-TCO is used to prepare EGFR-targeted and APN-targeted mRNA-loaded LNPs, mediating receptor-dependent endocytosis, mRNA delivery, and intestinal epithelial transcytosis.

Vicenin 2, a flavonoid, is an orally active angiotensin-converting enzyme (ACE) inhibitor (IC₅₀ of 43.83 μM). Vicenin 2 has radioprotective, anti-nociceptive effects, anti-glycation anti-inflammatory, antioxidant, anticancer, antiangiogenic properties.

Melatonin (Standard) is the analytical standard of Melatonin. This product is intended for research and analytical applications. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.

INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G₂-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway.

IBG1 is a bivalent molecular glue degrader targeting BRD2/BRD4, with IC₅₀ values of 12.8 nM and 462 nM, respectively, and an EC₅₀ of 44 nM. By binding to the adjacent BD1 and BD2 bromodomains of BRD2 and BRD4, IBG1 stabilizes the ternary complex formed with DCAF16, thereby driving CRL-mediated ubiquitination and proteasomal degradation. IBG1 induces cancer cell apoptosis and inhibits cancer cell growth in a DCAF16-dependent manner, and downregulates MYC expression through DCAF16-independent BET bromodomain inhibition. IBG1 can be used in research of various cancers including prostate cancer.