NERx 329 (RPAi 329, NERx329) is a novel potent, specific inhibitor of replication protein A (RPA), demonstrated potent RPA inhibitory activity in vitro, in vivo, and in cellular assays.

AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

NMS-P293 (also known as NMS-03305293) is an innovative, second-generation oral small molecule inhibitor specifically targeting PARP1. Developed by Nerviano Medical Sciences, it distinguishes itself from first-generation PARP inhibitors through its high selectivity for PARP1 over PARP2, which significantly reduces hematological toxicities like bone marrow suppression.A defining feature of NMS-P293 is its non-trapping mechanism; by inhibiting enzyme activity without trapping PARP on DNA, it offers a superior safety profile that allows for effective combination with DNA-damaging chemotherapies. Furthermore, it possesses exceptional blood-brain barrier (BBB) permeability, making it a leading candidate for treating primary CNS tumors like glioblastoma and brain metastases.

Novel selective inhibitor of the transient receptor potential melastatin 2 (TRPM2) channel, exhibiting TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showing neuroprotective activity in vitro, and significantly reducing ce

MS 177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

Novel Highly Selective Neuropeptide FF1 Receptor Antagonist, Potently Preventing Opioid-Induced Hyperalgesia

E3 ligase Ligand 1A is a ligand of E3 ligase, used in PROTAC technology; E3 ligase Ligand 1A can be used in the research of cancer. (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL)

VHL ligand 1 TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.

VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

Protac Linker 5 is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.

VH 032 Linker 6 is a derivative of the proteolysis-targeting chimera technology (PROTAC) for PROTAC research and development; by incorporating an E3 ligase ligand and a PEG2 linker with terminal alkyne, it is ready for conjugation to a target protein ligand

TL13-112 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of LDK378 and the cereblon ligand pomalidomide.

BAY-1797 is a potent and selective P2X4 antagonist.

Novel potent and selective PROTAC degrader of BRD3/4

TPCK is a non-specific irreversible inhibitor of serine/cysteine proteases. It acts by inhibiting ScRce1 in the presence of a Ras reporter, but not in the presence of the a-factor peptide.

Anandamide, also known as N-arachidonoylethanolamine or AEA, is a fatty acid neurotransmitter derived from the non-oxidative metabolism of eicosatetraenoic acid (arachidonic acid) an essential ω-6 polyunsaturated fatty acid. The name is taken from the Sanskrit word ananda, which means "joy, bliss, delight", and amide. It is synthesized from N-arachidonoyl phosphatidylethanolamine by multiple pathways. It is degraded primarily by the fatty acid amide hydrolase (FAAH) enzyme, which converts anandamid.

AC2P36 is a novel inhibitor of Mycobacterium tuberculosis (Mtb), selectively killing Mtb at acidic pH and potentiating the bactericidal activity of isoniazid, clofazimine, and diamide.

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

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM.

DMPAC-Chol is a cationic cholesterol derivative that has been used in liposome formation for gene transfection. Liposomes containing DMPAC-chol bind to DNA in a band shift assay and protect against serum nuclease degradation of DNA.

TL12-186 is a multikinase degrading PROTAC.

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.

DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells. DMHAPC-Chol, as part of a lipoplex with DOPE, has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to deliver VEGF siRNA into A431 and MDA-MB-231 cells, which secrete VEGF.

SJF-1521 is a selective EGFR PROTAC degrader. SJF-1521 is capable of inducing EGFR degradation in OVCAR8 cells. SJF-1521 can be used for tumor research.

Biotin alkyne for the preparation of various biotinylated conjugates via Click Chemistry. This alkyne reacts with various azides, including biomolecules containing azide groups. Biotinylated conjugates can be used for various assays and applications requiring affinity binding. Our recommended protocol can be used for the conjugation.

OTX-015 is a new potent BRD2/3/4 inhibitor with evident anti-proliferative activity in several cell lines representative of mature B-cell tumors.

E3 ligase Ligand-Linker Conjugates 17 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.

M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).