BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.

ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).

Crebinostat is a novel cognitive enhancer that inhibits class I HDAC/1/2/3 (IC50=0.7/1.0/2.0 nM), class IIb HDAC6 (IC50=9.3 nM) with weaker inhibition of the class I HDAC8 and no significant inhibition of the class IIa HDAC/4/5/7/9; potently induces acetylation of both histone H3 and histone H4 as well as enhanced the expression of the CREB target gene Egr1 in cultured mouse primary neurons; upregulates Bdnf and Grn, and downregulates Mapt (tau) gene expression-genes; brain penetrant.

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis.

QUN97653, also known as TBK1/IKKε-IN-5, is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. QUN97653 was first reported in patent WO 2016049211. It has CAS#1893397-65-3 without code name. For the convenience of scientific communication, we temporally name it as QUN97653, which was based on Hodoodo Chemical Nomenclature (https://hodoodo.com/hodoodo-chemical-nomenclature).

Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.

GNE-781 is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.

TPX-0022 (CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.

BIBO 3304 is a potent, selective, nonpeptide neuropeptide Y Y1 receptor antagonist with IC50 of 0.38 and 0.72 nM for human and the rat Y1 receptor, respectively.

PFM01 (SML1735) is a small molecule that specifically inhibits endonuclease, but not exonuclease activity of MRE11, inhibits dsDNA end resection in A549 cells with IC50 of 50-75 uM, blocks the ssDNA-binding path toward the catalytic metal ions and disrupt

LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1).

RAD51-IN-17 is a quinazolinone derivative that inhibts homologous recombinase RAD51, effectively inhibits both RAD51 foci formation in response to DNA damage, and proliferation of TNBC cell lines.

BRM/BRG1 ATP Inhibitor-1 is an orally active inhibitors of Brahma Homolog (BRM)/SMARCA2 with IC50 below 0.005 µM.

N-Acetyl-Calicheamicin is a enediyne antitumor antibiotic.

Norbergenin, the O-demethyl derivative of bergenin, shows moderate antioxidant activity (IC50 13 μM in DPPH radical scavenging; 32 μM in superoxide anion scavenging).

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.

11R-VIVIT is a potent NFAT inhibitor. 11R-VIVIT inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). 11R-VIVIT also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. 11R-VIVIT improves symptoms in a mouse model of colitis. Exhibits immunosuppressive effects; enhances graft survival in mice.

NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor.

Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.

Inhibitor of of the metalloproteinase ADAM17; Inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage, blocking TACE as well as ADAM10

MLS 0263839 is a potent, specific inhibitor of the phosphatase PHOSPHO1 with IC50 of 0.14 uM, shows minimal cross-inhibition of TNAP and no inhibition of ENPP1 activity.

CPYPP is a small-molecule inhibitor of the Rac activator DOCK2 with IC50 of 22.8 uM (DOCK2DHR-2-mediated Rac GEF activity), inhibits DOCK2-Rac1 interaction.

Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation. Lobaplatin has activity in a wide range of preclinical tumour models and appears to overcome tumour resistance to cisplatin and carboplatin in some of these models. In the body, lobaplatin remains largely intact until removed by glomerular filtration.

AY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. This may cause cell cycle arrest and induce apoptosis, which may lead to a reduction in tumor cell proliferation.

Mobocertinib succinate is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. TAK-788 exhibits antitumor activity in pts with EGFR exon 20 insertions with an AE profile consistent with other EGFR TKIs.

Lascufloxacin, also known as KRP-AM-1977, is a potent antibacterial drug candidate. Lascufloxacin showed a broad spectrum of activity against various clinical isolates. Especially, lascufloxacin showed the most potent activity against gram-positive bacteria among the quinolones tested. Furthermore, lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin showed potent inhibitory activity against both wild-type and mutated target enzymes. Lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM.