OPC-21268 is a vasopressin 1 receptor antagonist potentially for the treatment of heart failure and hypertension.

Bay K-8644 is a potent L-type calcium channels (LTCCs) activator with EC50 of 17.3 nM, has positive inotropic, vasoconstrictive and behavioral effects in vivo.

Dp44mT is a potent iron chelator, which shows selective antitumor activity.

Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.

Pico145 is a highly potent, subtype-selective TRPC1/4/5 channels inhibitor with potency ranged from 9 to 1300 pM, depending on the TRPC1/4/5 subtype and activation mechanism.

POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.

A highly potent, selective, orally available Src family kinase inhibitor with IC50 of <0.5 nM, <0.5 nM and for Src, Yes and Fyn kinases respectively, >950-fold selectivity for Src over ABL.

Traumatic Acid is a monounsaturated dicarboxylic acid isolated from  Phaseolus vulgaris. Traumatic Acid can cause a decrease in membrane phospholipid peroxidation and show antioxidant and stimulatory effects on collagen biosynthesis. Traumatic Acid is a potential agent for the treatment of many skin diseases connected with collagen biosynthesis disorders and oxidative stress.

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.

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.