VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.

Potent and specific pan-PIM inhibitor, inhibiting proliferation of several AML cell lines, showing dual antitumoral and bone antiresorptive effects

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).

MGH-CP1 is a potent and selective TEAD palmitoylation inhibitor.

iBAP-II (BAP1 inhibitor II) is a next-generation, specific small molecule inhibitor of BAP1 histone H2A deubiquitinase activity with IC50 of <0.1 ug/mL.iBAP-II displays higher affinity for BAP1 than the closest UCH family member, UCHL5, and other deubiquitinases, such as USP5, USP7, USP8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3.Inhibition of BAP1 via iBAP-II reduces ASXL3 protein stability in small cell lung cancer cells, without significant changes to ASXL1 and ASXL2 protein levels.iBAP-II suppresses ASCL1 expression in NCI-H1963 cells, along with the mRNA levels involving a handful of known ASCL1 transcriptional targeted genes, such as GRP, DMPK, RNF183, SCN3A, MYCL, and CACNA1A.iBAP-II exhibited more potent cell viability inhibition activity on four different BAP1-WT SCLC cell lines than iBAP.iBAP-II (50 mg/kg/d) significantly delayed the disease progression in SCLC xenograft model.

F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.

Lateritin is An Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor and a platelet aggregation inhibitor isolated from the mycelial cake of Gibberella lateritium; bassiatin is the (3S,6R) isomer.

TED-347 (TED347) is an irreversible inhibitor of TEAD4-Yap1 protein-protein interaction (EC50=5.9 uM in FP asssays) via covalent modification of conserved cysteine (Cys367, Ki=1.3 uM), inhibits its binding to Yap1, blocked its transcriptional activity.

BTT-266 (BTT266) is a voltage-gated CaV2.2 calcium channel inhibitor that disrupts the CaVα·CaVβ3 protein-protein interaction, directly binds to CaVβ3 with Kd of 3.6 uM.

ML090 (ML-090, CCG-44699, Fluoflavin, NSC 179821) is a potent, selecitve inhibitor of NADPH oxidase 1 (NOX1) with IC50 of 90 nM, displays no significant activities against NOX2, 3 and 4 (IC50>10 uM)..

Novel TDP-43 ligand, binding to TDP-43's RRM1 and RRM2 domains, partially disrupting TDP-43's interaction with the hexanucleotide RNA repeat of the disease-linked c9orf72 gene, improving larval turning, an assay measuring neuromuscular coordination and st

SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research.

WJ460 is one of the lead compounds exerting anti-metastatic activity in the nanomolar range in breast cancer cells.

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.

SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and cell cycle arrest and has in vitro efficacy in mantle cell lymphoma, hepatocellular carcinoma and neuroblastoma models.SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.

PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent.

MIF098 is a macrophage migration inhibitory factor (MIF) antagonist. MIF098 inhibits proliferation, migration and fibrosis of pulmonary smooth muscle cells. MIF098 can be used for immunoinflammation-related disease research.

Selective inhibitor of NADPH oxidase activity in low micromolar concentrations, interfering neither with ROS detection nor with XOD or eNOS activities

Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way.

OAT-2068 is a potent, selective, orally bioavailable inhibitor of mouse chitotriosidase (mCHIT1) with IC50 of 29 nM, 143-fold selectivity over mAMCase.

PHPS1 is an inhibitor of the protein tyrosine phosphatase Shp2. PHPS1 also efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

ZLc002 (ZLc-002) is a putative small-molecule inhibitor of nNOS interaction with NOS1AP, disrupts neuronal nitric oxide synthase-NOS1AP interaction in intact cells.

HaloPROTAC3 is a degrader of HaloTag fusion proteins.

Erastin is a compound that interacts with VDAC, blocked and reversed mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers.

11R-VIVIT TFA is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy.

Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.

Haloperidol lactate is a potent antipsychotic agent. Haloperidol lactate can be used in acute and chronic schizophrenia and gilles de la tourette's syndrome. Haloperidol lactate has the potential for the research of psychotic disorders.

USP10 inhibitor Wu-5 (Wu-5) is a novel small molecule USP10 inhibitor inducing the degradation of FLT3-mutated protein, directly interacts and inactivates USP10, the deubiquitinase for FLT3-ITD in vitro (IC50=8.3 uM) and in FLT3-ITD-positive AML cells.Wu-5 selectively inhibited the viability of FLT3 inhibitor-sensitive (MV4-11, Molm13) and -resistant (MV4-11R) FLT3-ITD-positive AML cells with IC50 of 3.794, 5.056, and 8.386 uM, respectively.Wu-5 (1-10 μM) dose-dependently induced apoptosis of MV4-11, Molm13, and MV4-11R cells through the proteasome-mediated degradation of FLT3-ITD.Combined treatment of Wu-5 and crenolanib produced synergistic cell death in FLT3-ITD-positive cells via the reduction of both FLT3 and AMPKα proteins.

Novel SIRT6 activator, significantly inhibiting the proliferation and migration of pancreatic ductal adenocarcinoma (PDAC) cells in vitro and markedly suppressing the tumor growth in a PDAC tumor xenograft model

Novel fluorescent substrate for both the serotonin transporter and the vesicular monoamine transporter 2 (VMAT2)