INR119 is a small molecule allosteric MAPKK (MAP2K, MEK1/2) inhibitor, binds fission yeast homologue Wis1 near C458 and protects Wis1 from inactivation by low levels of H2O2 in vitro.INR119 pretreatment strongly potentiates the Wis1 response to low H2O2 in vivo.Phosphorylation of Sty1 depends entirely on activated Wis1, and the INR119-induced enhancement of Sty1 pathway activation upon H2O2 stress requires the upstream activation of Wis1 through the MAPKKKs.

inhibitor of the human soluble epoxide hydrolase

PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity.

B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC50 value of 11.08 μM, which can be used in cancer-related research.

MMP-9-IN-7 is a potent MMP9 inhibitor with an IC50 of 0.52 μM in proMMP9/MMP3 P126 activation assay. MMP-9-IN-7 is extracted from patent WO2012162468 (example 59), and can be used for MMP9/MMP13 mediated syndrome research.

anti-dengue virus infections;

β-pBrPh-Glc is a small-molecule ice recrystallization inhibitor. β-pBrPh-Glc can control the rate and extent of intracellular ice recrystallization in the nuclei over a broad range of subzero temperatures. β-pBrPh-Glc is an important tool to improve the recovery and function of cryopreserved cells and tissues.

5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.

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 (BAP1 inhibitor I) is a first-in-class inhibitor of the catalytic activity of BAP1 histone H2A deubiquitinase complex with IC50 of 0.5-1 uM in vitro,

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.

2-Fluorofumarate is a bioactive chemical.

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)..

2-Amino-8-oxononanoic acid HCl is a biochemical

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.