ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.ETC-168 acts as a MNK2-biased, dual-MNK inhibitor in cells.ETC-168 induced dose-dependent growth suppression and inhibited 50% of cell viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.ETC-168 effectively suppressed both p-4E and cell viability in MESSA cells, but not CGP57380 and eFT508.ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS cell, decreased expression of E2F1, FOXM1, and WEE1.Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.

PAQ (Compound 4c) is a quinoxaline derivative. PAQ is an orally active neuroprotective agent, which targets dopamine (DA) neurons and activates reticulum endoplasmic ryanodine receptor (RyR) channels, without effects on glia cells.

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

C902 is a small-molecule inhibitor targeting LIN28-let-7 interaction, shows dose-dependent inhibition in an EMSA validation assay with IC50 of 5 uM.

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.

KA2507 (KA-2507, KA 2507) is a potent and selective inhibitor of HDAC6 with IC50 of 2.5 nM, >300-fold selectivity over other HDACs.KA2507 demonstrated cellular potency (IC50=150 nM) in a cellular assay measuring induction of acetylated α-tubulin, a marker of HDAC6 inhibition.KA2507 displays antiproliferative effects against a set of 93 human cancer cells with IC50 of 2-30 uM.KA2507 inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

Picotamide is a combined inhibitor of thromboxane A2 (TxA2) synthase and receptor. Picotamide has antiplatelet activity. Picotamide promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques in diabetes. Picotamide can be used for researching acute or chronic cardiovascular diseases.

ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively.

OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported.

Potent TIR1 antagonist, blocking the formation of the TIR1-IAA-Aux/IAA complex and so inhibiting auxin-responsive gene expressionReferences:1) Smékalová V, Luptovčiak I, Komis G, Šamajová O, Ovečka M, Doskočilová A, Takáč T, Vadovič P, Novák O, Pechan T,

Novel inhibitor of SIRT6, sensitizing pancreatic cancer cells to gemcitabineREFERENCES1) Damonte P, Sociali G, Parenti MD, Soncini D, Bauer I, Boero S, Grozio A, Holtey MV, Piacente F, Becherini P, Sanguineti R, Salis A, Damonte G, Cea M, Murone M, Poggi

Robenacoxib is a nonsteroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the relief of pain and inflammation in cats and dogs, a Cyclooxygenase(COX)-1 and COX-2 inhibitor..

SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ.

Inhibitor of histone deacetylase (HDAC); potently inhibits affinity purified HDAC1. Also inhibits the growth of tumor cells in vitro and in vivo. Induces p21/WAF1 expression in tumor cells.

Lalistat 2 is a specific inhibitor of lysosomal acid lipase (LAL) with no effect on other forms of lipase.

OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family.

6-Maleimidocaproic acid contains a maleimide group and a terminal carboxylic acid. The terminal carboxylic acid can be reacted with primary amine groups in the presence of activators (e.g. EDC, or DCC) to form a stable amide bond. The maleimide group will react with a thiol group to form a covalent bond, enabling the connection of biomolecule with a thiol.

NOX-6-18 is a potent, selective GPR132 antagonist with IC50 of 17 nM.

CPI-360 is a compound in design and preparation of wew palladium precatalysts for C-C and C-N cross-coupling reactions.

AG1478 HCl is an inhibitor of epidermal growth factor receptor protein.

MitoBloCK-10 (MB-10) is a potential attenuator of protein import into mitochondria via targeting Tim44, inhibits the import of substrates that use the TIM23 import pathway.

NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.

BVDV IN-1 is a non-nucleoside inhibitor of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM.

GAK inhibitor 49 is a potent, selective, ATP-competitive inhibitor of cyclin G-associated kinase (GAK, cell IC50=56 nM) with favourable NAK family selectivity (AAK1, STK16, BMP2K).

Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.