ER-000444793 is a potent, cyclophilin D-independent inhibitor of mitochondrial permeability transition pore (mPTP) with with IC50 of 2.8 uM.

Hydroxy-dabrafenib is one of the three major metabolites of dabrafenib.

Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.

MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments, confers growth in media lacking uracil in a specific manner and affects zebrafish development.

TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..

BAL3833 (also known as CCT3833) is an orally available small-molecule panRAF/SRC kinase inhibitor targeting cell proliferation signaling pathways that are associated with tumor growth and resistance development to current therapies. Data from preclinical studies suggest that this class of compounds, targeting the BRAF, CRAF and SRC family kinases, is active in diverse patient-derived melanoma models with intrinsic or acquired resistance to currently marketed BRAF-specific as well as MEK inhibitor therapies.8 Moreover, activity of BAL3833 has also been demonstrated in KRAS-driven cancer models, including non-small cell lung cancer, colorectal cancer and pancreatic cancer.9 BAL3833 has been progressed into a phase 1 study in adult patients with advanced solid tumors including metastatic melanoma.

Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..

ML417 is a Highly Selective D3 Dopamine Receptor Agonist. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors. Screening of ML417 against multiple G protein-coupled receptors revealed exceptional global selectivity. Molecular modeling suggests that ML417 interacts with the D3R in a unique manner, possibly explaining its remarkable selectivity. ML417 was also found to protect against neurodegeneration of dopaminergic neurons derived from iPSCs.

NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.

AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.

STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist.

MYCMI-6 (NSC354961) is a selective, high affinity inhibitor of MYC-MAX interaction, blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with Kd of 1.6 uM in SPR assay.

BL-918 is a small molecule activator of ULK1 with EC50 of 24 nM (243% kinase activity at 100 nM), induces autophagy via the ULK complex in SH-SY5Y cells.

1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.

MYCi361, also known as NUCC-0196361, is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 suppresses tumor growth and enhances anti-PD1 immunotherapy.

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.

GS-143 is an inhibitor of IκBα ubiquitylation. It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.

ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.

A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.

DSP-4 hydrochloride (Neurotoxin DSP 4 hydrochloride) is a highly selective neurotoxin and readily passes the blood-brain barrier with neurotoxic effects on noradrenergic neurons of adult and developing rats, can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons, mainly those from the locus coeruleus (LC).

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.

TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity[1][2].

CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein[1].

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.

LolCDE-IN-1 is an inhibitor of the Lol proteins (LolCDE) complex, with antibacterial activity.

HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases. HCH6-1 is a selective FPR1 inhibitor and has protective effects against acute lung injury (ALI). HCH6-1 inhibits superoxide anion generation, elastase release, and chemotaxis in human neutrophils activated by fMLF (an FPR1 agonist).

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors.