Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor..

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1).

γ-Amanitin an ADC cytotoxin and isolated from the?mushroom. γ-Amanitin inhibits?RNA polymerase II and disrupts synthesis of?mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin .

Inarigivir (ORI-9020) ammonium is a dinucleotide antiviral drug which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) act as an RIG-I agonist to activate cellular innate immune responses.

A4250 (A-4250, Odevixibat) is a small molecule ileal bile acid transporter (IBAT) inhibitor for the treatment of cholestatic liver diseases including progressive familial intrahepatic cholestasis and NASH..

Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia..

Exherin (ADH-1) trifluoroacetate is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities; selectively and competitively binds to and blocks N-cadherin.

Eptifibatide, also co-promoted by Schering-Plough/Essex, is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). It belongs to the class of the arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide has a short half-life. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody abciximab and the non-peptide tirofiban entered the global market.

Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate), a prodrug of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole L-lysine ethanolate can be used for candidiasis, onychomycosis and parasitemia research.

Antitubercular agent-30 is an antibacterial agent against Mycobacterium tuberculosis (MIC=50 μg/mL). Antitubercular agent-30 has little cytotoxic effect on murine macrophage cells (LD85=~100 μg/mL).

Vc-MMAD consists the ADCs linker (Val-Cit) and potent tubulin (MMAD). Vc-MMAD is a drug-linker conjugate for ADC.

VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM..

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).

CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.

Sec61-IN-1 is a potent sec61 inhibitor (Patent WO2020176863A1, compound A317).

SEP-363856 hydrochloride (SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia.

Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively.

Cysteine Thiol Probe is a thiol-based probe designed to label electrophilic natural products. Cysteine Thiol Probe possesses each of the characteristics of an ideal pharmacophore probe, and has a chromophore. Cysteine Thiol Probe is capable of engaging enone-, β-lactam-, and β-lactone-based electrophilic metabolites.

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

5'-O-DMT-2'-O-TBDMS-N-Bz-Adenosine is an adenosine derivative and can be used as an intermediate for oligonucleotides synthesis.

Potent aryl hydrocarbon receptor (AhR) ligand

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).

PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDKs are serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation and are frequently overexpressed in tumor cells. CDK2/cyclin E complex plays an important role in retinoblastoma (Rb) protein phosphorylation and the G1-S phase cell cycle transition. CDK2/cyclin A complex plays an important role in DNA synthesis in S phase and the activation of CDK1/cyclin B for the G2-M phase cell cycle transition.

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.

CAD-031 (CAD31) is a novel brain penetrant, J147-derivative that has enhanced neurogenic activity over J147 in human neural precursor cells (NPCs).

AA92593 has been used as a selective inhibitor of melanopsin.

Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.