SKS-927 is a Src kinase inhibitor, with an IC50 value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC50 value of 73 nM. SKS-927 exhibits an IC50 value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.

EMD 86006 is a candidate for selective serotonin inhibitors. EMD 86006 has the potential for research on depressive disorders.

CGP-79807 is a purine-based CDK inhibitor. CGP-79807 can block the cell cycle by inhibiting CDK activity to suppress the proliferation of tumor cells. CGP-79807 can be used in the study of cancer.

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.

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.

RAGE406R is an orally active RAGE-DIAPH1 interaction antagonist. RAGE406R can bind to ctRAGE and prevent the formation of the RAGE-DIAPH1 complex and inhibit its interaction. RAGE406R can reduce the expression of CCL2, TNF, and IL-6 in THP1 cells. RAGE406R suppresses delayed-type hypersensitivity in T2D mice. RAGE406R can be used for the study of diabetes.

Lotixparib (Example 1) is an inhibitor of poly(ADP-ribose)polymerase-1 (PARP-1). Lotixparib has cytoprotective effect against a retinal disease. Lotixparib can be studied in research for PARP-1-associated diseases.

W-255348 is an effective non-steroidal progesterone receptor (PR) antagonist that acquires antagonist activity by binding to and subsequently blocking progesterone induced nuclear accumulation, phosphorylation, and PR promoter interactions. WAY-255348 can be used in the research of reproductive disorders or PR-positive breast cancer.

BMS-779333 is an orally active androgen receptor (AR) antagonist. BMS-779333 is promising for research of prostate cancer and seizure.

RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research.

NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research.

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.

ALG-001075, a capsid assembly modulator (CAM), is an orally active HBV inhibitor. ALG-001075 effectively blocks not only HBV DNA production but also extracellular HBsAg/HBeAg and intracellular HBV RNA in primary human hepatocytes. ALG-001075 shows pronounced reductions of circulating HBV DNA in the AAV-HBV mouse model. ALG-001075 can be used for the study of Chronic hepatitis B (CHB).

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.

DH03 (6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-ethoxyquinoline-3-carbonitrile) is a SARS-CoV-2 MPro ligand. DH03 can be used as a Ligand for Target Protein for PROTAC synthesis, such as PROTAC SARS-CoV-2 Degrader-1.

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.

Z52 is a Ras protein inhibitor. Z52 can be used for the research of cancer, such as pancreatic cancer.

Z52-L16 is Drug-Linker Conjugates for ADC, which is composed of a linker and a Ras inhibitor Z52. Z52-L16 can be used for the research of cancer, such as pancreatic cancer.

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.

MTP3 ligand-1 is a MTP3 ligand for PROTAC MTP3 degrade-1. PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader.

MTP3 Ligand-linker Conjugate 1 is a conjugate of the MTP3 ligand and the linker. MTP3 Ligand-linker Conjugate 1 can be used for synthesis of PROTAC MTP3 degrade-1.

CRBN ligand-186 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.

BBH-4 is a SARS-CoV-2 major protease (MPro) inhibitor. BBH-4 can be used in SARS-CoV-2 infection research.

Trabectedin derivative 1 TFA is a selective DNA minor groove binder. Trabectedin derivative 1 TFA inhibits DNA transcription and repair to induce tumor cell apoptosis. Trabectedin derivative 1 TFA is promising for research of solid tumors such as soft tissue sarcoma and ovarian cancer.

BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites.

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).