Cancer Targeted Therapy

(E/Z)-OSM-SMI-8 ((E/Z)-NSC642624) is the racemate of OSM-SMI-8 (HY-148693). OSM-SMI-8 is an oncostatin M (OSM) inhibitor with a pK_i of 44.82 nM against human targets. OSM-SMI-8 inhibits the activation of STAT3, JNK, ERK 42/44 and AKT signaling pathways induced by OSM. OSM-SMI-8 is applicable to research related to cancer metastasis and Crohn's disease.

TASK-1-IN-1 is a potent and selective TASK-1 (Potassium Channel) inhibitor with an IC50 of 148 nM. TASK-1-IN-1 shows a reduced inhibition of TASK-3 channels (IC50 of 1750 nM) and not a significant effect on other K+ channels. TASK-1-IN-1 has anticancer effects.

NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)).

F1-RIBOTAC is a ribonuclease-targeting chimeras (RIBOTACs). F1-RIBOTAC decreases QSOX1-a mRNA expression level in an RNase L-dependent manner. F1-RIBOTAC can be used for the research of cancer. (Pink: RNA ligand (HY-168460); Black: linker (HY-W008005); Blue: RNase L ligand (HY-168452))

SLF TFA is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC₅₀ of 2.6 μM for FKBP12. SLF TFA can be used in the synthesis of PROTAC.

Azido-PEG11-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG11-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

JAK-IN-35 (compound XLVII) is a JAK2 inhibitor that canb be used in cancer research.

hsa-miR-4476 inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. Enocitabine inhibits the replication of human cytomegalovirus. Enocitabine has antileukemic and antiviral activities.

Amg-1 is a potent, reversible and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor (IC₅₀ = 3.0 μM). Amg-1 exhibits >80-fold selectivity over IDO2 (IC₅₀ > 250 μM) and >20-fold selective over TDO (IC₅₀ > 62.5 μM). Amg-1 can be used for cancer, hypotension, and neurological disorders research.

Aminooxy-PEG2-BCN is a cleavable PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-PEG2-BCN is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

Zavondemstat (QC8222; TACH 101) L-lysine is an orally active pan-KDM4 inhibitor, with a IC₅₀ ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat L-lysine induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat L-lysine suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat L-lysine can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer.

HO-PEG17-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

FTO-IN-3 is a FTO inhibitor that impair self-renewal in glioblastoma stem cells.

Eliroptamig is a multispecific antibody targeting albumin, folate receptor α (FOLR1) and cluster of differentiation 3 (CD3). Eliroptamig extends its half-life by binding to albumin, while targeting FOLR1 on tumor cells and activating T cells to achieve precise tumor killing.

Thalidomide-4-O-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

hsa-miR-15a-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC₅₀=17.2 nM).

Efbalropendekin Alfa (XmAb24306) is an IL-15/IL-15 receptor alpha complex fused to a heterodimeric Fc domain (IL15/IL15Rα-Fc). Efbalropendekin Alfa increases direct and antibody-dependent cellular cytotoxicity (ADCC)-mediated human natural killer (NK) cell cytotoxicity in vitro.

KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC₅₀s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer.