KY-9 is an antibacterial active compound.

(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.

BAS00602705 is an E-cadherin inhibitor. BAS00602705 exerts its function by blocking the trans-interactions of E-cadherin molecules within junctional complexes, without permanently altering E-cadherin expression levels. BAS00602705 significantly impairs invadopodia formation in pancreatic cancer cells. BAS00602705 can be used for the study of anti-invasive therapeutic strategies in cancers characterized by dysregulated E-cadherin-mediated invadopodia activity, such as pancreatic ductal adenocarcinoma (PDAC).

(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.

CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948.

TBIA (trans bis-isatoic anhydride) is a covalent RNA crosslinker. TBIA selectively induces RNA tertiary interactions (e.g., multi-helix junctions, loop-helix packing). TBIA is promising for research of RNA higher-order structure and disease-associated RNAs (e.g., KRAS-mutant RNAs).

(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

Ciprokiren (Ro 44-9375) is a Renin inhibitor with IC50s of 0.07 and 0.65 nM for hRenin in buffer and plasma, respectively. Ciprokiren be applied transdermally with similar hemodynamic effects without decrease of plasma renin activity or plasma immunoreactive angiotensin II. Ciprokiren has antihypertensive efficacy and can be used for hypertension research.

SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.

NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.

WB156 is a dual MDM2 and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia.

ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.

RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2)(IC50=100 nM). RJG-2036 inhibits NADPH-dependent reduction, significantly reducing secretion of proinflammatory cytokines like TNF-α and multiple eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 is promising for research of inflammatory diseases.

JSZ16 is a Succinate dehydrogenase (SDH) inhibitor with an IC50 of 30.3  μM. JSZ16 has potent broad-spectrum fungicidal activity, such as Sclerotinia sclerotiorum, Botrytis cinerea and Colletotrichum fragariae, with an EC50 of 4.4 mg/L for Sclerotinia sclerotiorum. JSZ16 influences the cell membrane permeability of pathogenic fungi. JSZ16 can be used for the development of fungicide.

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.

SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.

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.

BTR2038 is a BRD9 degrader. BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function.

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.

CGR-50 is a potent RSV fusion glycoprotein (F protein) inhibitor (EC50 = 32.6 nM against RSV A2 in HEp-2 cells). CGR-50 blocks RSV entry by binding to the F protein and inhibiting membrane fusion. CGR-50 can be used for RSV infection research.

4SC-207 is a potent, orally active microtubule inhibitor. 4SC-207 inhibits microtubule growth to inhibit tumor cell proliferation in vitro and in vivo, and promotes a mitotic delay/arrest, followed by apoptosis or aberrant divisions. 4SC-207 inhibits tumor growth in taxane resistant xenograft mouse models. 4SC-207 can be used for cancer research, such as colon adenocarcinoma and other malignancies.

Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

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.

ACP3 ligand 1 (compound I11a) is a ligand against Acid Phosphatase 3 (ACP3, ACPP). ACP3 ligand 1 interacts with ACP3 expressed on the surface of tumor cells for in vivo pharmaco-delivery applications.

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.