Androgen receptor ligand 1 is an androgen receptor (AR) ligand. Androgen receptor ligand 1 binds to CRBN E3 ligase via a linker to form an AR PROTAC degrader. Androgen receptor ligand 1 can be used in the study of prostate cancer.

(S)-AZD0022 is an isomer of AZD0022, AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.

N-Succinimidyl 3-maleimidopropionate (Compound MC1) is a Glucuronide-Gemcitabine conjugate. N-Succinimidyl 3-maleimidopropionate can be used to synthesize ADCs (such as cAc10ec-MC1). N-Succinimidyl 3-maleimidopropionate can be used in Hodgkin's lymphoma research.

NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).

Davalomilast (Example 100) is an PDE4 inhibitor with anti-inflammatory property. Davalomilast can be studied in research for autoimmune diseases and dermatology research.

SM311 (Compound 10), a chemical probe, is a potent selective irreversible LIMK1 inhibitor (EC50=0.045 μM, >30-fold selective over LIMK2). SM311 blocks cofilin phosphorylation and actin cytoskeleton regulation. SM311 is promising for research of neurodegenerative diseases like Fragile X syndrome (FXS) and Alzheimer’s disease, as well as tumor invasion.

X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).

CP-800569 is an orally active cholesteryl ester transfer protein (CETP) inhibitor. CP-800569 can decrease low-density lipoprotein and postprandial triglyceride and increase high-density lipoprotein. CP-800569 can be used for the research of metabolic disease.

Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer.

Comtifator (Example 77) is a modulator of the integrated stress response pathway. Comtifator can be studied in research for diseases associated with integrated stress response.

SB-219994 is a peroxisome proliferator-activated receptors (PPARs) agonists. SB-219994 can inhibit airway neutrophilia and associated chemoattractants/survival factors. SB-219994 exhibits anti-inflammation effec.

17β-HSD5 inhibitor 2 (Compound 30) is an inhibitor for 17β-hydroxysteroid dehydrogenases 5 (17β-HSD 5) with IC50 of 40 nM.

BTX-6654 (formate) is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 (formate) reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.

BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).

CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases.

AR ligand 42 is a androgen receptor ligand. AR ligand 42 can be used to synthesize androgen receptor PROTAC degrader ITRI-90.

TFSeB is an orally active neuroprotective agent. TFSeB can reduce Streptozotocin (STZ)-induced MAO-B and AChE activity. TFSeB exerts neuroprotective effects by increasing the expression of BCL-2, BDNF, NRF2, and decreasing the expression of BAX. TFSeB can reduce lipid peroxidation (TBARS) and reactive oxygen species (ROS) levels. TFSeB can reduce neuroinflammation. TFSeB can be used for research on Alzheimer’s disease.

Gemigliptin (hydrochloride) is the hydrochloride salt of Gemigliptin. Gemigliptin (hydrochloride) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin (hydrochloride) exhibits potent anti-glycation properties. Gemigliptin (hydrochloride) can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.

Lenacapavir pacfosacil (Example 44) is a viral capsid and nucleocapsid inhibitor. Lenacapavir pacfosacil has antiviral effects. Lenacapavir pacfosacil can be used for research of Retroviridae infection, including an HIV infection.

C3TD078 is a WDR5 WIN site inhibitor with a Ki of 0.03  nM. C3TD078 has potent antiproliferative activity and reduces the stem-cell frequency of cancer stem cells (CSCs). C3TD078 can be used for glioblastoma (GBM) research.

(-)-2-Fluorodeoxyarbutin is a fluorinated derivative of the tyrosinase inhibitor deoxyarbutin.

(+)-2-Fluorodeoxyarbutin is a fluorinated derivative of the tyrosinase inhibitor deoxyarbutin.

Maleimide-Ph(3,5-F)-PEG4-Val-Ala is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).

Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 is a drug-linker conjugate for ADC. Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 consists of a topoisomerase 1 inhibitor (Topi MF-6)175203) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala). Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 can be used for synthesis of ADCs.

Eratrectinib (Example 1) is a Trk inhibitor. Eratrectinib can be studied in research for tropomyosin receptor kinase-related diseases and cancers.

K2V-9 is an AChE and MAO-B inhibitor with IC50 values of 1.72 μM and 0.950 μM against AChE and MAO-B, respectively. K2V-9 inhibits amyloid β self-aggregation and reduces ROS. K2V-9 has neuroprotective effects.

RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD).

Pan-KRAS ligand 3 is a pan-KRAS inhibitor. Pan-KRAS ligand 3 can be used for synthesis of PROTAC pan-KRAS degrader-1.

Naperiglipron (LY3549492) (Example 2) is a Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.