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.

TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.

BTK ligand 16 is a BTK ligand that can be used for synthesis of TQ-3959.

(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.

JPS004 is a HDAC1-3 PROTAC degrader. JPS004 can induce degradation of HDAC1-3 and induce histone acetylation. JPS004 can induce cancer cells apoptosis. JPS004 can be used for the research of cancer.

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).

OICR-41103N is the negative control form of OICR-41103. OICR-41103 is an effective, selective, cell-active DCAF1 small molecule chemical probe (Ki<2 nM) that targets the DCAF1 WDR domain and replaces the viral Vpr protein.

OICR-41103 is an effective, selective, cell-active DCAF1 small molecule chemical probe that targets the DCAF1 WDR domain and replaces the viral Vpr protein. The binding Ki value of OICR-41103 and DCAF1 is less than 2 nM.

(S,S,S)-AHPC-Me is an E3 ligase ligand. (S,S,S)-AHPC-Me can be used for synthesis of PROTAC (4S)-PROTAC SOS1 degrader-1 diTFA.

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.

FLT3/CHK1 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC FLT3/CHK1 Degrader-1. PROTAC FLT3/CHK1 Degrader-1 is a potent FLT3/CHK1 PROTAC degrader with anti-tumor activity.

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.

IAP ligand 5 is a IAP ligand. IAP ligand 5 can be used to synthesize PROTAC ERα Degrader-2.