TEAD-IN-24 (Example 65) is a TEAD inhibitor. TEAD-IN-24 exhibits anti-cancer activity against non-small cell lung cancer.

TEAD-IN-23 (Compound 22) is an efficient pan-TEAD inhibitor with an IC50 of 10 nM. TEAD-IN-23 exhibits potent anti-proliferative activity in both NCI-H226 and MSTO-211H. TEAD-IN-23 causes complete tumor regression in the MSTO-211H xenograft tumor model. TEAD-IN-23 can be used for the study of mesothelioma and hepatocellular carcinoma.

Tazolol is a specific β-adrenergic antagonist (IC50: 700 nM for (-) isoproterenol-elicited accumulation of cyclic AMP in rat cortical slices). Tazolol produces a significant and sustained increase in cardiac output and stroke volume. Tazolol can be used in the research of heart failure.

Tau ligand-2 is a tau aggregate ligand with a Ki value of 0.99 nM. Radiolabeled (18F) Tau ligand-2 serves as a PET tracer. Tau ligand-2 is applicable to research related to Alzheimer's disease.

Tagorizine is a 5-LOX inhibitor. Tagorizine can be used to study cerebral (or peripheral) blood vessel dilation.

TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.

SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC50 of 89 pM and a Ki of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression.

Sulofenur (LY186641) is an orally active anti-tumor agent. Sulofenur induces gene expression through calcium ion-dependent pathways and some protein kinase-independent pathways, and its effect is particularly enhanced in H-ras mutant cells. Sulofenur exhibits significant activity in mouse solid tumor models and human tumor xenograft models.

STING-IN-17 (compound 10a) is an orally active STING (human STING IC50 = 29 nM, mouse STING IC50 = 15 nM) inhibitor. STING-IN-17 can inhibit the phosphorylation of STING, TBK1 and IRF3. STING-IN-17 dose dependently inhibits the mRNA expression of IP10, IFNB1 and ISG56. STING-IN-17 can reduce ROS and inhibit the expression of cleaved-PARP/caspase-3. STING-IN-17 can improve kidney function. STING-IN-17 can be used for research on inflammatory conditions such as acute kidney injury.

STING agonist-48 is a potent STING agonist that exhibits STING-dependent activity in vitro (EC50 = 4.02 μM). STING agonist-48 prefers to bind with the transmembrane domain (TMD) over the cytosolic cyclic dinucleotide (CDN) domain. STING agonist-48 shows adjuvant efficacy, enhancing IgG and Th1/Th2 cytokine responses in humanized STING mice. STING agonist-48 can be used for the study of inflammation-related diseases.

Stibophen is a potent antiparasitic agent is effective against Litomosoides carinii, Dipetalonema witei, and Brugia pahangi. Stibophen inhibits lactate accumulation and phosphofructokinases (PFK) activity in adult filariids. Stibophen also inhibits Ascaris and Hymenolepis diminuta PFK without inhibiting mammalian liver PFK. Stibophen can be used for the research of schistosomiasis and filariid infections.

STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer.

Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor, antinociceptive, anti-inflammatory, sedative, anxiolytic, and antimicrobial agent with oral effectiveness, IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coli RNase H, and >495 µM for human DNA polymerase β.Soulattrolide inhibits HIV-1 RT’s DNA-dependent and RNA-dependent DNA polymerase activities, E. coli RNase H activity, and Mycobacterium tuberculosis growth.Soulattrolide shows no activity against HIV-2 RT, AMV RT, RNA polymerase, or HIV-1 RTTyr181, and lacks antidepressant activity.Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection.

SNX3-IN-1 is a sorting nexin 3 (SNX3) inhibitor. SNX3-IN-1 reduces SNX3 protein expression and inhibits SNX3-mediated activation of the Wnt/β-catenin signaling pathway. SNX3-IN-1 inhibits the proliferation and migration of pulmonary fibrosis-related cells, and decreases the expression of fibrosis markers α-SMA and COL-1. SNX3-IN-1 can be used in research related to pulmonary fibrosis.

SMU-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research.

SMARCA2/4-ligand-7 is a SMARCA2/4 ligand, which can be used for the synthesis of PROTACs, such as PROTAC SMARCA2/4 degrader-41.

SLD1121 is an agonist of the Wnt/β-catenin signaling pathway that enhances Wnt signaling by targeting LRP6 (Kd: 4.52-7.49 nM). SLD1121 interacts with the intracellular domain of LRP6, stabilizes LRP6, promotes its nuclear translocation, and facilitates its binding to β-catenin, TCF4 or LEF1 in the nucleus, thereby inducing the expression of Wnt-regulated genes and stem cell-related genes. SLD1121 induces the transition of hair follicles from telogen to anagen in the mouse hair growth cycle and promotes hair growth in mice. SLD1121 is applicable to hair loss-related research.

SLC6A19-IN-4 is an allosteric-competitive and orally active B0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research.

SIRT6-IN-6 (compound 6d) is a potent and selective SIRT6 inhibitor with an IC50 of 4.93 μM and a Ki of ~10 μM. SIRT6-IN-6 shows selectivity against other members of the HDAC family (SIRT1-3 and HDAC1-11). SIRT6-IN-6 significantly increases the level of glucose transporter GLUT-1, thereby reducing blood glucose in a mouse model of type 2 diabetes. SIRT6-IN-6 can be used for type 2 diabetes research.

Simeconazole is a demethylation inhibitor-class fungicide. Simeconazole prevents the infection of barley leaves by Blumeria graminis f sp hordei, inhibits the development of powdery mildew on barley and cucumber leaves, and exhibits cuticular membrane permeability in tomato fruits. Simeconazole can be used in research related to barley powdery mildew and cucumber powdery mildew.

Sim-9 is a covalent allosteric inhibitor of interferon regulatory factor 3 (IRF3). Sim-9 binds covalently to the Cys222 residue of IRF3, induces its conformational change, blocks its interactions with TRIF, MAVS and STING, and inhibits IRF3 homodimerization and type I interferon response. Sim-9 exhibits significant anti-inflammatory, organ-protective and survival benefits in mouse models of sepsis and acute pancreatitis. Sim-9 can be used for research related to inflammatory diseases.

SIK2/3-IN-3 (Example 15) is a potent, selective SIK2/3 inhibitor that exhibits preferential inhibitory activity against SIK2 (IC50 = 10.3 nM) and SIK3 (IC50 = 0.8 nM) over SIK1 (IC50 = 801 nM). SIK2/3-IN-3 can be used for the study of inflammatory diseases.

SIK2/3-IN-2 (compound 12, compound I-200) is a potent SIK2/3 inhibitor (SIK2 IC50 = 65 nM, SIK3 IC50 = 14 nM). SIK2/3-IN-2 is also a p21-activated protein kinase (PAK) 1 inhibitor with a Ki of 20.7 nM. SIK2/3-IN-2 can be used for hyperproliferative diseases and cancer research, such as Paclitaxel-resistant ovarian cancer.

SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02. SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1.

SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis, and reduces the colony-forming ability of prostate cancer cells. SGI-1776-VHL-02 can be used in studies related to prostate cancer. (Pink: Pim and Autophagy and Apoptosis ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).

SET7-IN-DC21 is a selective, potent SET7 inhibitor (IC50 = 15.93 μM; KD = 18.00 μM). SET7-IN-DC21 has good selectivity for several other epigenetic targets, such as SUV39H1, G9a, NSD1, DOT1L and MOF. SET7-IN-DC21 can be used for the researches of cancer, infection, inflammation, metabolic and cardiovascular disease, such as breast cancer.

SDH-IN-45 is a succinate dehydrogenase BcSDH inhibitor and mycelial growth inhibitor targeting Botrytis cinerea, with an IC50 of 5.97 μg/mL against Botrytis cinerea. SDH-IN-45 inhibits succinate dehydrogenase, a component of the mitochondrial electron transport chain, via a unique binding mode, thereby regulating fungal energy metabolism. SDH-IN-45 causes morphological damage to Botrytis cinerea mycelia, leading to collapse and shrinkage of mycelial structures. SDH-IN-45 exhibits in vitro fungicidal activity against Botrytis cinerea. SDH-IN-45 can be used in research related to cucumber gray mold.

SDH-IN-44 is a succinate dehydrogenase (SDH) inhibitor with an IC50 of 12.5 μg/mL against Alternaria solani. SDH-IN-44 exhibits antifungal activity and inhibits fungal mycelial growth. SDH-IN-44 is applicable to research related to fungal infections.

SC-45662 is a 5-lipoxygenase inhibitor. SC-45662 inhibits the response of monocytes to phytohemagglutinin (PHA). SC-45662 inhibits superoxide production in neutrophils. SC-45662 slows early changes in lung mechanics and pulmonary hypertension in a sheep model of impaired lung function. SC-45662 can be used in research on diseases of the immune system, respiratory system, etc.

SB-773812 is a moderate-affinity antagonist at dopamine receptor 2 (pKi=7.4) and a high-affinity antagonist at the dopamine receptor 3 (pKi=8.5) and at the serotonin 5-hydroxytryptamine receptors 2A (pKi=9.0), 2C (pKi=8.1), and 6 (pKi=8.1). SB-773812 is promising for research of central nervous system disorders.