ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.

AP232 is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 can be used for the research of cancer, such as Leukemia.

Negamycin (hydrochloride) is a dipeptide antibiotic. Negamycin (hydrochloride) can restore dystrophin expression in skeletal and cardiac muscles in mdx Duchenne muscular dystrophy (DMD) murine model. Negamycin (hydrochloride) can bind to a partial sequence of the eukaryotic rRNA-decoding A-site. Negamycin (hydrochloride) can be studied in DMD research.

Ro 31-8220 formic is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Ro 31-8220 formic can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.

JBPOS-0101 is a phenyl carbamate compound. JBPOS-0101 exhibits neuroprotective and antiepileptic effects. JBPOS-0101 can attenuate the accumulation of Aβ in 5XFAD mouse brains and rescue the deficits in learning and memory. JBPOS-0101 can be used for the research of neurological disease, such as Alzheimer's disease (AD).

TXA497 is a potent local topical bactericide. TXA497 exerts its bactericidal effect by interfering with the polymerization kinetics of the bacterial cell division protein FtsZ, rather than inhibiting it. TXA497 shows strong activity against various Staphylococcus aureus strains, including MRSA and MSSA, with an MIC value ranging from 1.0 to 2.0 μg/mL. TXA497 skin deposition is concentration-dependent in its formulation, consistent with Fick's first law. TXA497 has limited systemic permeability through the lipid pathway of the stratum corneum and is easily absorbed through this route. TXA497 can be used for research on topical bactericidal agents.

FR-β ligand 1 (III), a folate receptor-targeting ligand, possesses antitumor activity, high selectivity, and stronger affinity for folate receptor.

Bis-Cl-ANT-ATP (tetrasodium) is a fluorescent ATP derivative, which undergo spontaneous isomerization. Bis-Cl-ANT-ATP (tetrasodium) selectively inhibits B. pertussis Adenylyl Cyclase (AC) toxin CyaA over mammalian AC1, AC2, and AC5 (Kis = 16, 1,700, 2,400, and 1,600 nM, respectively). Bis-Br-ANT-ATP (tetrasodium) can be used in the study of whooping cough.

Bis-Br-ANT-ATP (tetrasodium) is a fluorescent derivative of adenosine-5’-triphosphate (ATP). Bis-Br-ANT-ATP (tetrasodium) selectively inhibits B. pertussis adenylyl cyclase toxin CyaA (Ki: 12.6 nM). Bis-Br-ANT-ATP (tetrasodium) can be used in Whooping cough research.

KARI 201 hydrochloride is a selective, brain penetrant pand competitive acid sphingomyelinase (ASM) inhibitor with an IC50 of 338.3?nM. KARI 201 hydrochloride is a ghrelin receptor agonist. KARI 201 hydrochloride improves neuropathological features of Alzheimer's disease.

Basivarsen linker is a linker used in Zeleciment basivarsen for coupling a TfR1-binding Fab Zeleciment) and an antisense oligonucleotide. Zeleciment basivarsen is an antibody-oligonucleotide conjugate (AOC) designed to target mutant nuclear myotonic dystrophy protein kinase (DMPK) RNA for RHase H-mediated degradation to correct splicing. It is used for the study of myotonic dystrophy type 1 (DM1).

LY-228729 is a selective 5-HT1A receptor agonist. LY-228729 can reduce the rearing frequency of rats and decrease their activity in the central area in the open field test. LY-228729 can reduce the immobility time of rats and increase their swimming time in the forced swim test. LY-228729 can be used in the research of neurological diseases.

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.

U93385 is a 5-HT₁A receptor agonist. U93385 exhibits no significant α₂ adrenergic, D₂ dopamine, or other receptor activities. U93385 has a heart rate regulating effect, stimulating the vagus nerve to induce bradycardia. U93385 can be used to study the 5-HT₁A receptor-mediated vagal nerve tolerance mechanism.

(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.

Dicytidine 5′-triphosphate (Cp3C) is a cytosine-containing dinucleoside polyphosphate. Dicytidine 5′-triphosphate inhibits the intracellular accumulation of trans-resveratrol and trans-piceid. Dicytidine 5′-triphosphate induces the expression of CCR2 and upregulates the expression of PAL1 and 4CL1.

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).

MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma.

TD-6301 is a bladder-selective M2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M2/4 muscarinic receptors with high selectivity, especially human M2 receptors with strong affinity (Ki = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder.

BC264 is a highly potent and selective CCK-B agonist that crosses the blood-brain barrier. BC264 increases dopamine in the nucleus accumbens and facilitates motivation and attention in rats.

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.

BP 554 is a selective 5-HT1A receptor agonist and Piperazine derivative. BP 554 leads to hypothermia.

Guanidino ethyl disulfide (GED) (Compound 23) is a NO Synthase (NOS) inhibitor with EC50s of 110, 630 and 180  μM for iNOS, eNOS and bNOS, respectivly. Guanidino ethyl disulfide effectively inhibits nitrite production in J774.2 macrophages. Guanidino ethyl disulfide can be used for circulatory shock, inflammation and neurological diseases research.

S-0636 is a novel glutamyl cyclase (QC) inhibitor characterized by high selectivity, low cytotoxicity, and difficulty in inducing drug resistance. S-0636 can effectively inhibit the virulence factors of P. gingivalis. S-0636 can be used for research on bacterial infections.

DX-9065a (free base) is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a Ki of 41 nM for human FXa. DX-9065a (free base) has low activity against other serine proteases. DX-9065a (free base) has strong anticoagulant actions.

NAPAP is a thrombin inhibitor. It has potent antithrombin activity (Ki: 2.1 nM). NAPAP selectively inhibits thrombin via a rapid binding mechanism, and has weaker inhibitory effects on trypsin, factor Xa, and plasmin. NAPAP can be used in the study of thrombotic diseases (e.g., venous thrombosis, myocardial infarction).

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.