CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.

cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.

OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis.

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan in mice.

CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.

Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).

SUCNR1-IN-2 (Statement 35) is a succinate/succinate receptor 1 inhibitor for the study of neurodegenerative diseases such as neuroinflammation.

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a Ki of 8 nM against human Y5.

CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.

Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of Mebeverine. Mebeverine is an antispasmodic agent. Mebeverine acid is a valuable marker of oral exposure to Mebeverine.

HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells.

ATC0175 is a novel nonpeptidic and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.

Bevenopran is a peripheral μ-opioid receptor antagonist.

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

BB-22 is a third generation SPICE/K2 cannabinoid wih dopamine (DA) stimulant properties. BB-22 shows affinity to CB1 receptors with a Ki value of 0.11 nM and an EC50 value of 2.9 nM. BB-22 also stimulates CB1-induced [35S]GTPγS binding.

CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors.

Cotoin is a natural product isolated from the stem bark of Garcinia virgate.

PLpro-IN-1 (Compound 2) is a SARS-CoV PLpro inhibitor (IC50: 8.7 μM). PLpro-IN-1 can be used for antiviral research.

TAU-IN-1 (compound 051) is a TAU protein inhibitor with an EC50 value of 325 nM. TAU-IN-1 can be used in the study of neurodegenerative diseases.

AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.

GalNac-L96, the G-rich oligonucleotides carrying the longer GalNAc linker that can be used for delivery of nucleic acid drugs[1].

Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer.

CX-6258 HCl is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

WAY-213613 (hydrochloride) is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system.