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PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

SMS2-IN-1 is a potent and highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM and a Kd of 37 nM. SMS2-IN-1 shows 150-fold selectivity for SMS2 over SMS1 (IC50 of 1000 nM).

NSC-92828, also known as 3-Phenanthrenebutyric acid, is a Protein–protein interaction inhibitor (2P2 inhibitor or 2P2I). Protein–protein recognition is the cornerstone of multiple cellular and pathological functions. Therefore, protein–protein interaction inhibition (2P2I) is endowed with great therapeutic potential despite the initial belief that 2P2I was refractory to small-molecule intervention.

HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.

HMN-176 is a stilbene derivative which inhibits mitosis without significant effect on tubulin polymerization.

HTHQ, which is a hydroquinone monoalkyl ether, is a potent anti-oxidative agent, even at low dose levels.

hVEGF-IN-1 represses human VEGF-A translation and shows antitumor activity.

Hycanthone, the most potent mutagen in a series of nine thiaxanthenones, is a potent inducer of nuclear immunoreactivity to antinucleoside antibodies in HeLa cells.

Hydroxy-Fasudil is a metabolite of Fasudil, acting as a potent Rho-kinase inhibitor and vasodilator.

Hydroxyhexamide is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agents.

I-191 is a novel potent, selective protease-activated receptor 2 (PAR2) antagonist with pIC50 of 7.2 in cell-based assays.

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.

Icariside I is a metabolite of Icarlin, which could regulate bone remodeling and is recognized as an effective agent for the treatment of osteoporosis.

Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings.

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM).

IDE-2 is a cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 223 nM for induction of Sox17 expression in ESCs).

Importazole is an inhibitor of importin-β transport receptors.

Ingenol is an extremely weak protein kinase C (PKC) activator.

FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.

Irinotecan hydrochloride is the hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata.

Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

Valrubicin (AD-32) is a chemotherapy drug used to treat bladder cancer.

A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay).

CITCO is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.

AH-7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist.

Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.

A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays.