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.

MSU 38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth; MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream targets, including NQO1, GCLC, GCLM, AKR1C2, and UGT1A6. MSU38225 strikingly decreases the protein level of Nrf2, which can be blocked by the proteasome inhibitor MG132. Ubiquitination of Nrf2 is enhanced following treatment with MSU38225. By inhibiting production of antioxidants, MSU38225 increases the level of reactive oxygen species (ROS) when cells are stimulated with tert-butyl hydroperoxide (tBHP). MSU38225 also inhibits the growth of human lung cancer cells in both two-dimensional cell culture and soft agar.

N-Desmethyl Pimavanserin (AC-279) is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

AZD4747 is a highly potent and selective inhibitor of KRASG12C with IC50 of 15 nM. AZD4747 also shows an anticipated low clearance and high oral bioavailability profile in humans.

PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis.

CWI1-2 hydrochloride is an inhibitor of IGF2BP2 that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects.

CWI1-2 is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects.

T-518 (T518) is a potent, highly selective, brain penetrant, oral HDAC6 inhibitor with IC50 of 36 nM.T-518 did not obviously inhibit human HDAC1, 4, or 7 at 10 uM, which belongs to Class I or Class IIa HDAC.T-518 showed brain penetration in an oral dose and blocked HDAC6-dependent tubulin deacetylation at Lys40 in mouse hippocampus.T-518 decreased RIPA-insoluble tau accumulation (3-month treatment, 1 and 3 mg/kg), restored impaired axonal transport and novel object recognition in the P301S tau Tg mouse (tauopathy model) by 2-week treatment with dose 1 and 3 mg/kg.

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).

SG094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.

SC-9 is a PKC activator in the presence of Ca2+.

NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells were preincubated with NH-23-C2 inhibitor, MDM-2 cleavage was inhibited in a concentration-dependent manner (IC50 =3.11 μM).NH-23-C2 selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage.

SC-1 (1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea, STAT3-IN-7), a Sorafenib analogue and potently inhibits the phosphorylation of STAT3, induces cell apoptosis through SHP-1 dependent STAT3 inactivation.