PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]this compound for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications.

SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.

BIEGi-1 is a potent and selective binary inhibitor of EGFR that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR–Rheb interaction. It robustly inhibits both EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. This compound exhibits significant anti-proliferative effects with an IC50 of 17 nM for PC9 and 20 nM for HCC827.

BSJ-5-63 is a potent PROTAC degrader of CDK12, CDK7, CDK9. BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K, while also suppressing the mRNA expression of BRCA1 and BRCA2. BSJ-5-63 demonstrates anticancer properties and has the potential for the research of prostate cancer.

Emvistegrast is a quinolone derivative. Emvistegrast is an antagonist of α4β7 integrin. Emvistegrast can be studied in research for diseases that are mediated by α4β7 integrin, such as infkammatory bowel disease.

WEHI-7326 (WEHI 7326) is a specifi mitotic inhibitor and potential anticancer agent, causes cell cycle arrest in G2/M, cell death in vitro (MDA-MB-231 IC50=24.4 nM), and displays efficacious anti-tumor activity in vivo.WEHI-7326 induces cell death in a broad range of cancer cell lines, including taxane-resistant cells, and inhibits growth of human colon, brain, lung, prostate and breast tumors in mice xenografts.WEHI-7326 exceeded potency of myoseverin B by almost ten-fold, did not show any significant cytotoxic activity in vitro (IC50>40 uM) in HepG2 cells.WEHI-7326 prolongs survival in mouse models of high-risk neuroblastoma and leads to complete tumor regression when used in combination with standard-of-care relapse therapies.

N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.

A nonsteroidal selective estrogen receptor modulator (SERM) that shows 10- to 60-fold increased affinity for the estrogen receptor compared with Tamoxifen.

1400W dihydrochloride is a slow, tight binding, potent and highly selective inhibitor of inducible nitric oxide synthase (Kd = 7 nM).

Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way.

PSTC is a potent, selective Nrf2 activator with pEC50 of 7.7 (inducing of NQO1 specific enzyme activity).PSTC induces Nrf2 nuclear translocation, Nrf2-regulated gene expression, and downstream signaling events, including induction of NAD(P)H:NQO1 enzyme activity and heme oxygenase-1 protein expression, in an Nrf2-dependent manner.PSTC does not inhibit IL-1β-induced NF-κB translocation or insulin-induced S6 phosphorylation in human cells.PSTC restores oxidant (tert-butyl hydroperoxide) induced glutathione depletion in vitro and in vivo models of pulmonary oxidative stress.

MitoTracker Green FM is a green-fluorescent dye that can selectively accumulate in the mitochondrial matrix. MitoTracker Green FM covalently binds to mitochondrial proteins by reacting with free thiol groups of cysteine residues.

AGPS-IN-1a is a potent inhibitor of the ether lipid-generating enzyme alkyl-glycerone phosphate synthase (AGPS), selectively lowers ether lipid levels in several types of human cancer cells and impairs their cellular survival and migration..

AMXT-1501 tetrahydrochloride (AMXT 1501, AMXT1501) is a novel potent polyamine transport inhibitor, synergistically reduces cell viability in NB cells in combination with DFMO.

(S)-IBD3540 is a potent, gut-restricted and orally active small molecule glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 4 nM, demonstrates anti-colitis activity in both acute and chronic mouse colitis models.

A novel small molecule disruptor of HuR-mRNA interaction with Ki of 350 nM.

Camonsertib is a potent ATR inhibitor. ATR inhibitor 4 has antitumor activity.

DOIC is a cationic lipid that can be used for RNA vaccines.

DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells. DMHAPC-Chol, as part of a lipoplex with DOPE, has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to deliver VEGF siRNA into A431 and MDA-MB-231 cells, which secrete VEGF.

Novel free radical scavenger, against light-induced photoreceptor cell damage

BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.

OAT-1746 is a novel potent, selective, orally active inhibitors of Arginase 1 and 2 (ARG1/2) with IC50 of <50 nM.

Y-320 is a potent inhibitor of the STING with IC50 of 356 nM, approximately 8-fold more potent than the canonical STING inhibitor tool drug H-151. Y-320 blocks STING Golgi translocation and downstream signaling and dose-dependently ameliorates cisplatin-induced acute kidney injury in mice.

OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.

FG-0041 (FG0041) is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 2 uM for collagen prolyl hydroxylase.

C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.

HIV inhibitor, showing selective activity against human RNaseH2

Syn-TEF1 is a molecule actively enables transcription across repressive GAA repeats that silence frataxin expression in Friedreich's ataxia, license transcription elongation at targeted genomic loci.

CGX1321 (CGX-1321) is a nove potent and specific inhibitor of porcupine (PORCN) that inhibits Wnt pathway, block secretion of WNT proteins with IC50 of 1 nM; CGX1321 displayed >500 times selective for Porcupine over the most related target enzyme, hedgehog acyltransferase. CGX1321 increased Ki67+ and phosphohistone H3 (PH3+) cardiomyocytes in culture, up-regulated cell cycle regulating genes such as Ccnb1 and Ccne1, did not alter YAP protein phosphorylation and nuclear translocation in cardiomyocytes. CGX1321 administration blocked the secretion of Wnt proteins, and inhibited both canonical and non-canonical Wnt signaling pathways in MI injury mice. CGX1321 improved cardiac function, reduced myocardial infarct size, and fibrosis of post-MI hearts. CGX1321 significantly increased newly formed cardiomyocytes in infarct border zone of post-MI hearts, evidenced by the increased EdU+ cardiomyocytes.

T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD).