NED-3238 is highly potent third generation inhibitors of human arginase I and II with IC50 of 1.3 nM and 8.1 nM respectively.

PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.

SS-208 (SS208) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 12 nM, >100-fold selectivity over HDAC1/4/5/7/8/9/11.SS-208 has minimal effects on the viability of murine SM1 melanoma cells in vitro, significantly reduced in vivo tumor growth in a murine SM1 syngeneic melanoma mouse model.

GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.

XPC-6444 is an CNS-penetrant, isoform-selective NaV1.6 inhibitors with IC50 of 41 nM, which also displayed potent block of NaV1.2 with IC50 of 125 nM.

AT-001 is a nociceptin opioid receptor (NOP) partial agonist with Ki of 10.3 nM, which may be useful to develop nondopaminergic treatments for Parkinson's Disease.

AT-004 is a nociceptin opioid receptor (NOP) partial agonist with Ki of 9.8 nM, which may be useful to develop nondopaminergic treatments for Parkinson's Disease.

AT-035 is a nociceptin opioid receptor (NOP) partial agonist with Ki of 3.27 nM, which may be useful to develop nondopaminergic treatments for Parkinson's Disease.

BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced models (preclinical models of psoriasis).

MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.

ETX1317 is a novel broad-spectrum inhibitor of class A, C, and D serine β-lactamases.

X-165 is a highly potent, selective and bioavailable autotaxin inhibitor with IC50 of 12 nM in the autotaxin LPC enzymatic assay.

DS34942424 is an orally potent analgesic without mu opioid receptor agonist activity.

GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1.

BAY1217224 is a highly potent, orally bioavailable, neutral, non-prodrug thrombin inhibitor with IC50 of 0.7 nM.BAY1217224, has reached first clinical trials, which have confirmed the desired pharmacokinetic properties.

CG428 (CG-428) is a first-in-class potent and selective TRK degrader (PROTAC) with DC50 of 0.36 nM.CG428 (CG-428) showed selectivity for the degradation of endogenous TPM3-TRKA over ectopically expressed ATP/GTP binding protein-like 4 (AGBL4)-TRKB or ETS variant transcription factor 6 (ETV6)-TRKC fusion proteins in KM12 cells.CG428 exhibited higher potency for inhibiting growth of KM12 cells with IC50 of 2.9 nM, compared with the parental TRK kinase inhibitor.CG428 (CG-428) is a valuable chemical tool compound for investigating the in vivo function of TRK fusion during tumorigenesis

LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.

VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression.

VPC-18005 (VPC18005) is a novel small molecule ERG (ETS-related gene) antagonist that inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, disrupts the ERG binding to DNA (Kd=250 uM).

An STAT3 inhibitor that selectively targets the DNA-binding domain of STAT3, without affecting the activation and dimerization of STAT3.

I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).

BAY-091 is a novel potent and highly selective inhibitor of the kinase PIP4K2A.

MS8511 is a highly potent, selective, and cell-active covalent inhibitor of G9a (Kd=44 nM) and GLP (Kd=46 nM). MS8511 could be a useful chemical tool for investigating the physiological and pathophysiological functions of G9a and GLP.

LNP Lipid-1 (Method B) is a lipid compound. LNP Lipid-1 is involved in the synthesis of lipid nanoparticles compositions. LNP Lipid-1 has potential applications in the transport of biologically active substances such as small molecule drugs, proteins, and nucleic acids.

MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.

5,6-Dichlorobenzimidazole riboside is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. 5,6-Dichlorobenzimidazole riboside trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.

BDCRB (GW 275175) is a potent and selective inhibitor of human CMV replication by blocking the processing and maturation of viral DNA..

PF04802367 is a potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in vitro and in vivo.