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.

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

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.

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).

FBPase-1 inhibitor-1 (compound 1) is a novel allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1).

PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay.

BTYNB is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA with IC50 of 5 uM.

KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).

AS-1269574 is a selective, orally available GPR119 agonist with EC50 of 2.5 uM in cell-based cAMP assays.

UTL-5g is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity. It lowers elevated levels of AST, ALT, creatinine, BUN, and TNF-α, increases the reduced platelet count in mice, and acts as a novel chemo- and radioprotective agent.

UTL-5g (GBL-5g) is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity.

m-3M3FBS is an activator of phospholipase C (PLC). It acts by stimulating superoxide generation, Ca2+ release and inositol phosphate formation in a variety of cell types.

FIPI (5-Fluoro-2-indolyl des-chlorohalopemide) hydrochloride, a derivative of Halopemide (HY-119093), is a phospholipase D (PLD) inhibitor with IC50s of approximately 25 nM and 20 nM for PLD1 and PLD2, respectively. FIPI hydrochloride inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI hydrochloride has the potential for autoimmunity and cancer metastasis research.

BD-1047 is a potent, selecitve Sigma 1 receptor (σ1) antagonist with Ki of 0.93 nM.

Fatostatin A is a Cell permeable inhibitor of SREBP activation. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma.

XE-991 is a potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.

Quisinostat, also known as JNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation.

Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.

Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction.

Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure.

DB2313 is a small-molecule transcription factor PU.1 inhibitor abrogating DNA binding by PU.1 with Kd of 29 nM.

Novel mc (maleimidocaproyl) linker plus MMAD (Monomethylauristatin D) to be used for prepare antibodies conjugates via cysteine-capped mechanism

Val-cit-PAB-OH is a peptide prodrug linker.

SN34960 is a small molecule Perforin inhibitor, inhibits perforin-induced lysis of Jurkat T-lymphoma cells with IC50 of 6.65 uM, shows suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo.