Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.

ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.

Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.

Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1).

GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .

HDAC-IN-26 is a highly selective class I HDAC inhibitor with an EC50 value of 4.7 nM.

Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM.

Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer.

DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2'-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.

Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.

αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .

Sabarubicin is a doxorubicin disaccharide analogue with striking antitumor activity. Sabarubicin is more effective than doxorubicin as a topoisomerase II poison and stimulated DNA fragmentation at lower intracellular concentrations.

CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11).

Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.

Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease (extracted from patent WO2016200101A2).

PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.

Bersiporocin is a prolyl-tRNA synthetase inhibitor. Bersiporocin has an IC50 of ≤100 nM for phosphoribosylpyrophosphate synthetase (PRS). Bersiporocin can be used for the research of antifibrotic.

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25).

Deoxythymidine-5'-triphosphate (dTTP) sodium hydrate is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate trisodium salt is used in the synthesis of DNA.

EC2629 is a highly potent folate receptor (FR)-targeted DNA crosslinking agent. EC2629 can be used for the research of FR-positive tumors, including those that are classified as drug resistant.

Porfiromycin is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts.

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

Tinengotinib is the modulator of one or more protein kinases such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential for the research of these kinase abnormalities diseases mediated, especially cancer-related diseases (extracted from patent WO2018108079A1).

ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13).

N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity.

ATG7-IN-1 is a potent and selective inhibitor of ATG7 (IC50 = 62 nM).

TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα (KD = 6.8 nM).

TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.