E17110 is a liver X receptor β (LXRβ) agonist with an EC50 of 0.72 μM. E17110 can increase the expression of ATP-binding cassette transporter A1 (ABCA1) and G1 (ABCG1) in RAW264.7 macrophages. E17110 also reduce cellular lipid accumulation and promoted cholesterol efflux. E17110 can be used for the research of cardiovascular disease, such as atherosclerosis.

OncoFAP-GlyPro-MMAE is a FAP small molecule-drug conjugate (SMDC) with an IC50 of 0.49  nM. OncoFAP-GlyPro-MMAE consists of a FAP Ligand OncoFAP), a Tubulin inhibitor (MMAE) and a linker. OncoFAP-GlyPro-MMAE can be used for cancers like renal cancer research.

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma.

DF-003 is a selective, orally active, ATP-competitive, and brain-penetrant ALPK1 inhibitor. DF-003 potently inhibits human ALPK1 and ALPK1[T237M] with IC50s value of 1.5 nM and 16 nM. DF-003 exhibits more than 860-fold selectivity over the closest kinase. DF-003 inhibits TNF, CXCL10, or CXCL8 upregulation in HEK-293 cells. DF-003 can be used for the study of retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache (ROSAH) syndrome.

CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 inhibits cell migration and halts the cell cycle and induces apoptosis, significantly suppressing pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 can be used for the study of pancreatic cancer such as PDAC.

CL2A acid is a ADC linker for synthesis of Antibody-drug conjugates (ADCs)

TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver.

LAG-3 Hit II is a LAG-3 inhibitor with a KD of 4.32  μM. LAG-3 Hit II can be used for cancers like ovarian cancer, colon adenocarcinoma and melanoma research.

E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with Ki values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm.

(R)-CFMB is the R-enantiomer of CFMB). CFMB is an agonist of FFAR2- and FFAR3-specific with an EC50 value of 0.8 μM target hFFAR2 and 0.2 μM target rFFAR2.

PAD-PF1 is a PAD4 inhibitor (IC50: 15.9 µM). PAD-PF1 binds to an allosteric site of PAD-PF1, which is distinct from substrate and GSK147.

PAD-PF2 is a PAD4 inhibitor with a Kd of  2.82 µM. PAD-PF2 inhibits Ionomycin-induced protein citrullination in human isolated neutrophils.

ESC1002755 is a 17β-HSD10 inhibitor with an IC50 of 19 nM. ESC1002755 has significant enzyme specificity with non-/uncompetitive inhibition against the cofactor NADH. ESC1002755 shows minimal cytotoxicity towards the HEK293 at 50 μM. ESC1002755 is promising for Alzheimer’s disease and hormone-dependent cancers (such as prostate, bone and colorectal cancer) research.

Z88418521 is a ligand for the WDR5-MLL1 complex. Z88418521 may help disrupt the interaction of the WDR5-MLL1 complex. Z88418521 can be used in cancer research, especially in leukemia.

RIPK1 ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for RIPK1 and a PROTAC linker, which recruits E3 ligases. RIPK1 ligand-Linker Conjugate-1 can be used for synthesis of PROTAC RIPK1 Degrader-1

CDD-2210 is a STK33 inhibitor, with a Kd of 0.1 nM and an IC50 of 38 nM. CDD-2210 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 1209 nM for CLK1, 917 nM for CLK2, 544 nM for CLK4, and 746 nM for RET. CDD-2210 can be used for the study of contraception.

CDD-2212 is a STK33 inhibitor, with a Kd of 1.9 nM and an IC50 of 999 nM. CDD-2212 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 can be used for the study of contraception.

Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder.

CDD-2211 is a STK33 inhibitor, with a Kd of 0.018 nM and an IC50 of 5 nM. CDD-2211 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 115 nM for CLK1, 48 nM for CLK2, 187 nM for CLK4, and 78 nM for RET. CDD-2211 can be used for the study of contraception.

GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC50 values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma.

SUAM 1221 is a prolyl endopeptidase inhibitor. CS-0777 can be used in the research of Alzheimer diseases.

K-Ras ligand-Linker Conjugate 6 formate incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 formate can be used in the synthesis of PROTAC K-Ras Degrader-1), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.

MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).

tri(GalNAc-PEG2)-PEG4-cyclo(Ac-DCAW-{Arg(3F-Ph)-PEG2}-LGELVWCT) (Cys2-Cys12) is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

MC-Gly-Gly-Phe-OSu is an ADC linker. MC-Gly-Gly-Phe-OSu can be used for the research of cancer.

BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer.

JW 618 is a selective ABHD6 inhibitor, with IC50s of 38 and 13 nM for mouse and rat ABHD6.

MNFA is a derivative of Monofluoroacetic acid. MNFA is an effective pesticide.

FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels.

4-DTM-phenoxy-PEG4-CH2COOH (Formula 3) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).