tert-Butyl 4-(azetidin-3-yl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

tert-Butyl 3-(piperazin-1-yl)azetidine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

tert-Butyl (3-(methylamino)propyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.

tert-Butyl (2-(azetidin-3-yl)ethyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.

Ternidazole is a 2-methyl-5-nitroimidazole derivative and an antiprotozoal agent. Ternidazole exhibits antiprotozoal properties and is found to be effective against chronic alcoholism.

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.

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.

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.

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.

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.

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.

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.

SB-201993 is a selective leukotriene B₄ (LTB4) receptor antagonist with a Ki=7.6 nM for LTB4 receptors on human inflammatory cells. SB-201993 inhibits calcium mobilization in inflammatory cells and 5-lipoxygenase activity, exerting anti-inflammatory effects. SB-201993 is promising for research of inflammatory diseases (e.g., dermatitis, arthritis).

SARS-CoV-2 PLpro-IN-7 (Compound 18) is a selective SARS-CoV-2 PLpro inhibitor with an IC50 of 13.3 μM. SARS-CoV-2 PLpro-IN-7 exerts antiviral activity against SARS-CoV-2 (with an EC50 of 11 μM for SARS-CoV-2 in Huh7.5 cells). SARS-CoV-2 PLpro-IN-7 is applicable to research related to COVID-19.

SARM1-IN-9 (Compound MY-13B) is a stereoselective SARM1 inhibitor. SARM1-IN-9 is applicable to research related to axon degeneration-dependent neurological diseases.

Sapunifiram is a cognitive enhancer. Sapunifiram can be used in studies related to amnesia.

Saccharolactone is a potent orally active β-glucuronidase inhibitor. Saccharolactone markedly lowers biliary endogenous β-glucuronidase activity in the rat bile. Saccharolactone can stabilize glucuronide metabolites in vitro. Saccharolactone is also a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC50 < 4 mM).

Rosellichalasin is an antibacterial agent isolated from the endophytic fungus Aspergillus flavipes Y-62. Rosellichalasin exhibits antibacterial activity.

RIG 200 is an S-nitrosothiol nitric oxide (NO) donor. RIG 200 releases NO through decomposition, activating guanylate cyclase (sGCM) in vascular smooth muscle cells, increasing cGMP levels, and leading to vasodilation. RIG 200 significantly inhibits Collagen-induced platelet aggregation in platelet-rich plasma (PRP). RIG 200 may be used in research on antithrombus.

RhlR agonist-1 is a N-acylated L-homoserine lactone and is a selective quorum sensing receptor RhlR agonist. RhlR agonist-1 can be used for the research of bacterial infections.

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RETWT, RETV804L, RETV804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.

Quizalofop-p-tefuryl is an aryloxyphenoxypropionate herbicide. Quizalofop-p-tefuryl exhibits medium-high persistence in distilled water.

Quilostigmine (HP-290) is an orally active Physostigmine analogue, acetylcholinesterase (IC50: 148 nM for rat brain acetylcholinesterase) inhibitor. Quilostigmine has a long-lasting effect on tremors. Quetiapine can be used in the research of Alzheimer's disease.