Irafamdastat (BMS-986368) (Example 74) is a FAAH and MAGL inhibitor, with IC50s ≤ 100 nM (human FAAH) and 100 nM-1 μM (human MAGL) respectively. Irafamdastat has antiepileptic effect.

(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg. Bexobrutideg is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase.

Tacedinaline-C9-acid is a HDAC1-3 ligand-Linker conjugate. Tacedinaline-C9-acid can be used to synthesize HDAC1-3 PROTAC degrader JPS004.

RSL3-NH2 is a GPX4 inhibitor and Ferroptosis inducer. RSL3-NH2 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).

Mal-G(PEG8-Me)-AAN-NH2 is a linker of the drug conjugate QHL-1618. QHL-1618 has anti-tumor activity.

Ledasorexton (Example 1 ) is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect.

SRI 31215 is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitory activity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer.

APC8696 is a reversible uPA inhibitor, with a Ki of 8 nM.

Exatecan-3-amine is an effective exatecan derivative. Exatecan-3-amine can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan-3-amine is often combined with CLDN6 mAb to form ADC drugs for the study of tumors with high expression of CLDN6.

c-Met ligand-Linker Conjugate 2 is a synthesized target protein ligand-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC c-Met degrader-6. PROTAC c-Met degrader-6 is a c-Met PROTAC degrader with anti-tumor activity[1].

TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer.

SGC-CK1γ-1 is a potent and selective probe for the CK1γ subfamily. SGC-CK1γ-1 can inhibit LRP6 phosphorylation levels. SGC-CK1γ-1 can selectively inhibit the CK1γ kinases in living cells and inhibit both WNT signaling and human cytomegalovirus (CMV) replication. SGC-CK1γ-1 can be used for the research of infection.

MEK4 IN-3 (Compound 39) is a selective MEK4 inhibitor with IC50s of 78   and 2920 nM for MEK4 and RSK4, respectively. MEK4 IN-3 reduces toxicity in cells. MEK4 IN-3 can be used for liver failure, particularly nonalcoholic fatty liver disease (NAFLD) research.

P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM). P-gp inhibitor 30 promotes apoptosis , induces autophagy,and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research.

K-5a2 is the non-isotopic form of ZK-316. ZK-316 is a potent and broad-spectrum NNRTI inhibitor with an EC50 value ranging from 0.99 to 75.1 nM. ZK-316 can be used in the study of HIV.

GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases.

Angexostat (Compound 2) is an inhibitor of xanthine oxidase. Angexostat exhibits high permeability. Angexostat inhibits CYP2C9 with an IC50 of 18.1 μM. Angexostat can be studied in research for xanthine oxidase-related diseases such as hyperuricemia and gout.

KR30031, a Verapamil analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting P-gp with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer.

PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [68Ga]Ga to form [68Ga]Ga-PSMA-DIM. [68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa).

Tpl2 Kinase Inhibitor 1 hydrochloride is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 hydrochloride plays an important role in the regulation of the inflammatory response and the progression of some cancers.

QNX-10 is a fatty acid synthase (FASN) inhibitor (IC50 = 0.7 μM) with anticancer activity. QNX-10 exhibits potent FASN inhibition and cytotoxicity against colorectal and breast cancer cells. QNX-10 induces apoptosis and cell cycle arrest in S phase by upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-xL. QNX-10 can be used to investigate anticancer therapies targeting FASN enzymes.

CSBP ligand 1 (Compound 36) is a ligand of CSBP, with an IC50 of 0.08 μM for CSBP binding. CSBP ligand 1 can inhibit the production of TNF in mice treated with LPS. CSBP ligand 1 has no significant inhibitory activity against PGHS-1 (IC50: 16 μM) and 5-LO (IC50: 60 μM). CSBP ligand 1 can be used in the research of inflammation-related diseases.

3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid is a target protein ligand-linker conjugate that incorporates a ligand for c-Met and a PROTAC linker, which recruits E3 ligases. 3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid can be used in the synthesis of PROTACs, such as SJF-8240

KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc.

Anion transporter-4 (Compound 6) is a small-molecule anion transporter, which induces tubulin degradation and mitochondrial dysfunction. Anion transporter-4 can increase intracellular anion levels such as chloride ions by disrupting microtubule dynamics, promoting lipid peroxidation, and impairing mitochondrial function. Anion transporter-4 triggers ferroptosis to exert anticancer activity. Anion transporter-4 is promising for research of cancers.

OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research.

ELQ-453 is an inhibitor targeting the Qo site of the Plasmodium falciparum cytochrome bc1 complex (CytB) with an IC50 value of 0.57 nM. ELQ-453 blocks the mitochondrial function of the parasite, and suppresses Plasmodium infection in mosquitoes. ELQ-453 is promising for research of malaria.

AZD3839 (fumarate) is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 (fumarate) inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 (fumarate) inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 (fumarate) binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 (fumarate) can be used in the field of Alzheimer's disease research.

LP-65 is a dual inhibitor of MEK (IC50=83.2 nM) and mTOR (IC50=40.5 nM). LP-65 blocks MEK and mTOR signaling pathways and inhibits tumor cell proliferation and migration. LP-65 is promising for research of cancers.

Cleminorexton (Compound 67A) is an agonist of orexin-2 receptor (OX2R). Cleminorexton can be studied in research for narcolepsy and other disorders related to orexin insufficiency and/or excessive sleepness.