Novel, systemically active kynurenine aminotransferase 2 (KAT2) inhibitor, significantly decreased escape latency in the Morris water maze, indicating improved performance in spatial and contextual memorynovel

Alprenolol HCl, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris. It is no longer marketed by AstraZeneca, but may still be available from other pharmaceutical companies or generically.

A potent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload an

PF 6260933 is a potent, selective and orally bioavailable MAP4K4 inhibitor with kinase IC50 of 3.7 nM, cell IC50 of 160 nM.

Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. It reduces glucose and body weight, and has the potential to be used in Type 2 diabetes mellitus (T2DM) research.

GNE-684 is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

BAY-850 (BAY 850, BAY850) is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay.

H3B8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WT or mutant SF3B1 (binding IC50 of 0.3-2 nM),demonstrates dose-dependent inhibition of both canonical splicing and aberrant splicing induced by mutant SF3B1 in in vitro assays of biochemical splicing, induces lethality in spliceosome-mutant cancer cells.. H3B-8800 potently and preferentially kills spliceosome-mutant epithelial and hematologic tumor cells.

UNC-1679 (UNC1679) is a potent and selective small molecule chemical probe of a methyl-lysine reader protein L3MBTL3 with Ki of 0.35 uM.

Vamorolone (VBP-15) is a dissociative steroidal compound, reduces NF-κB-mediated cytokine expression in vitro, alsp reduecs glucocorticoid-mediated side-effects when compared to dexamethasone in vivo.

Boc-Val-Cit-PAB is a linker for Antibody-Drug-Conjugation (ADC). The Val-Cit will specifically be cleaved by catepsin B. As this enzyme is only present in the lysosome the ADC payload will be release only in the cell. The Boc group can be deprotected under acidic conditions to generate a free amine group.

PESTAHIVIN is a cell adhesion molecule inhibitor. HUN-7293 selectively inhibits the expression of three cell adhesion molecules (VCAM-1, ICAM-1 and E-selectin) (IC50=1-24 nM). HUN-7293 can be used in the study of inflammatory and autoimmune diseases characterized by overexpression of cell adhesion molecules.

Trofinetide (NNZ-2566) is an analog of a molecule which is derived from IGF-1 and occurs naturally in the brain. IGF-1 is a growth factor stimulated by growth hormone.

(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).

GSK 3011724A (DG-167, GSK-3011724A) is a potent, specific inhibitor of β-ketoacyl-ACP synthase (KasA, Kd=9 nM), shows anti-tubercular activity (MIC H37Rv=0.8 uM); shows much weaker apparent dissociation constant for both Pks10 and Pks (Kd=1.4 uM); inhibits mycolic acid biosynthesis and shows negligible activity against a panel of unrelated proteins and 18 Gram-positive and Gram-negative bacterial species.

DJ4 (ROCK inhibitor DJ4) is a potent, selective, ATP-competitive inhibitor of ROCK1/2 and MRCKα/β with IC50 of 5/50 nM and 10/100 nM, respectively.

BDT001 is a first-in-class, non-competitive FLT3 negative allosteric modulator, effectively prevents extracellular cytokine FL binding to FLT3 with IC50 of 11 uM.

K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.

(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation.

M4K2209 is a potent, selective BMP type I receptor ALK2 inhibitor with IC50 of 9 nM, >180-fold selective over ALK5 (IC50=2427 nM).

NCGC2955 is a Novel Inhibitor of Human Cytomegalovirus (HCMV)

BAY-598 is a selective inhibitor of SMYD2.

DB213 (RG-501) is a small molecule stimulator of HIV-1 frameshifting and inhibitor of viral replication.

SLU-PP-332 is a potent, selective pan ERRα/β/γ agonist with EC50 of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, in full-length ERR cell-based cotransfection/reporter assays.

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100  μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins. AD-5591 is the active form of AD-9308.

ZINC 17988990 is a potent, selective inhibitor of TRPV5 mediated currents, inhibits rbTRPV5/hTRPV5 with IC50 of 106/177 nM, showing marked selectivity for TRPV5 over TRPV6.ZINC 17988990 shows no activity on other TRP channels (TRPV1, TRPV3, TRPV4 and TRPM8) at 1-3 uM, and moderate inhibition on TRPV3 and TRPM8 at >10 uM.ZINC17988990 (10 uM) fully inhibited Ca2+ signals elicited by application of external Ca2+ in HEK293 cells transfected with TRPV5, but had no effect in cells expressing TRPV6.

INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 μM). INT-777 mitigates inflammatory response in human endometriotic stromal cells: A therapeutic implication for endometriosis.