TDI-6118 is a potent, selective brain-penetrant EZH2 inhibitor with IC50 of 14 nM, inhibits cellular H3K27me with IC50 of 580 nM.

TDI-11904 is a highly potent, and peripherally active EZH2 inhibitor.

TC-6683 (AZD1446) is a potent and highly selective α4β2 nAChR agonist with Ki of 30/34 nM against hα4β2/rα4β2, with little to no affinity against h α3β2 and h α7 (Ki>6.7 uM).TC-6683 (10 uM) produced <30% inhibition of specific binding or enzyme activity at all targets except the human (87%) and murine (97%) 5-HT3 receptors at a panel of 70 receptors, ion channels, and enzymes at NovaScreen/Caliper.TC-6683 (AZD1446) enhanced working memory in the object recognition paradigm in rats at every dose tested (0.1−3 mg/kg, po), exhibited favorable pharmaceutical properties and in vivo efficacy in animal models.

TC-5115 (TC5115 ) is a potent, selective inhibitor of MLL1 SET domain with IC50 of 15 nM, 48 times more potent than the pan-methyltransferase inhibitor SAH.

tatM2NX is a novel potent, selective, cell permeable, peptide TRPM2 channel antagonist with IC50 of 396 nM, IC90 of 2 uM (TRPM2 channel currents), prevents ligand binding and TRPM2 activation.tatM2NX interacts with the ADPR binding site on the NUT9-H domain of TRPM2 channel. tatM2NX inhibits TRPM2-mediated dephosphorylation of GSK3β (activation), tatM2NX demonstrated selective neuroprotective effects in a mouse model of focal ischemia (stroke).

TAT-K-tetracosapeptide is K-tetracosapeptide fused to a cell-permeable TAT peptide, K-tetracosapeptide (K-TC) is a peptide of 24 amino acids corresponding to the helix a5 in KRAS4B, potent inhibitor of KARATE.TAT-K-tetracosapeptide blocks insulin-induced phosphorylation of AKT and its downstream effector TBC1D4, a Rab GTPase-activating protein.TAT-K-tetracosapeptide strongly inhibits insulin-induced transport of GLUT4-GFP to the plasma membrane and glucose uptake in adipocytes.

TASP0410461 is a potent, selective histamine H3 receptor antagonist/inverse agonist.

Targapremir-200c (TGP-200c) is a structure-specific, small molecule inhibitor of miR-200c precursor (pre-miR-200c), binds to the Dicer site of pre-miR-200c with Kd of 50 nM.TGP-200c inhibits Dicer processing of pre-miR-200c with IC50 320 nM, selectively engages pre-miR-200c in cells.TGP-200c potently inhibits miR-200c biogenesis selectively across the miRnome and modulates the downstream miR-200c pathway.TGP-200c selectively inhibits miR-200c over other miR-200 family members by recognizing the 1x1 UU internal loop unique to pre-miR-200c and an adjacent AU base pair simultaneously.TGP-200c selectively rescues a miR-200c-mediated phenotype in MIN6 cells, induces anti-apoptotic phenotype, modulates various T2D-related pathways, including insulin signaling and metabolism, represses pro-cell death factors and promotes β cell survival in specific ways.

SYHA1815 (SYHA-1815) is a novel potent, selective RET inhibitor, inhibits the kinase activity of RET wild type (IC50=0.9 nM) and V804 mutant (IC50=3.1 nM).SYHA1815 demonstrated approximately 20-fold selectivity for RET over KDR, exhibited a favorable selectivity profile, with> 100-fold selectivity over 347 kinases, and >10-fold selectivity over 44 other kinases in a panel of 395 kinases.SYHA1815 significantly inhibited RET phosphorylation and activation of its key adaptor protein SHC and the downstream signaling molecules p-AKT and p-ERK1/2 in classical RET mutant-driven MTC cell line TT (RETC634W), effectively inhibited p-RET, p-SHC, and downstream p-AKT and p-ERK activity.SYHA1815 inhibited RET-induced cell proliferation and overcame V804 mutants (TT cell proliferation IC50<1.6 nM), suppressed RET-driven cell proliferation via cell-cycle arrest through c-Myc downregulation.SYHA1815 showed potent antitumor efficacy against RET- and RET gatekeeper mutant-driven cancers in vivo.

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).SY-5102 (SY5102) displays highly selectivity against CDK2, CDK9, and CDK12 (all IC50>75 nM).SY-5102 potently inhibits HCC70 cell proliferation with EC50 of 9 nM.SY-5102 showed dose-dependent tumor growth inhibition including tumor regression at 4 mg/kg po (dosed twice daily) in an HCC70 cell line derived xenograft mouse model.

SY2-062 is a thalidomide derivative and useful precursor for synthesis of thalidomide-based PROTAC degrader.

SW2_152F (SW2 152F) is a potent, selective, cell permeable CBX2 chromodomain probe, binds to the N-terminal chromodomain (ChD) with Kd of 80 nM.SW2_152F displays 24-1,000-fold selectivity for CBX2 ChD over other CBX paralogs (CBX4/6/7/8) in vitro.SW2_152F is cell permeable, selectively inhibits CBX2 chromatin binding in cells, and blocks neuroendocrine differentiation of prostate cancer cell lines in response to androgen deprivation.

SW-101 (SW101) is a potent, selective HDAC6 inhibitor with IC50 of 0.7 nM, >200-fold selectivity over HDAC1/2/3.SW-101 possesses excellent HDAC6 potency and selectivity, together with markedly improved metabolic stability and druglike properties compared to SW-100.SW-101 treatment elevates the impaired level of acetylated α-tubulin in the distal sciatic nerve, counteracts progressive motor dysfunction, and ameliorates neuropathic symptoms in a CMT2A mouse model bearing mutant MFN2.

SW IV-52 is a pro-apoptotic small molecule SMAC mimetic and XIAP inhibitor.

SW IV-134 is a sigma-2/SMAC drug conjugate, chemically linked the sigma-2 ligand SW43 to the Smac mimetic SW IV-52.SW IV-134 slowed tumor growth and improved survival in murine models of pancreatic cancer.SW IV-134 significantly reduced tumor burden and improved overall survival in a mouse xenograft model of ovarian cancer without causing significant adverse effects to normal tissues.SW IV-134 induced degradation of cIAP-1 and cIAP-2 leading to NF-қB activation and TNFα-dependent cell death.

SU086 is an inhibitor of HSP90, binds to HSP90-alpha and HSP90-beta isoforms, decreases HSP90 protein levels in prostate cancer cells.SU086 is a potent inhibitor of prostate cancer cell growth, migration, and invasion in vitro, significantly inhibited growth of AR-positive CRPC cell lines (C4-2), AR-negative (DU145 and PC-3) CRPC cells, and CRPC cells with expression of AR and AR splice variant, AR-V7 (22Rv1) (IC50 <10 uM).SU086 inhibits prostate cancer growth in preclinical models of prostate cancer in vivo.SU086 strongly enhances the anti-tumor activity of standard of care second-generation anti-androgens enzalutamide and abiraterone and inhibits prostate cancer cell growth in vitro and tumor growth in vivo.

STS66 is a novel BBB-penetrant NKCC1 inhibitor.STS66 treatment completely blocked the ischemia-induced elevation of pNKCC1, which is superior to BMT and STS5.STS66 showed efficacy against permanent focal ischemic brain injury with hypertension comorbidity.

STING agonist 22 is a novel, non-nucleotide specific small-molecule STING agonist with IC50 of 28, 11 uM for human STING isoforms WT and HAQ, respectively.STING agonist 22 did not show any cytotoxicity in an immune cell proliferation panel across a variety of immune cell types and also did not show any activity in a kinome panel.STING agonist 22 introduced higher levels of iFIT3 and MX1 mRNA across three different donors possessing different STING genotypes: WT/WT, WT/HAQ, and WT/R232H in human PBMCs (IC50=5-35 uM).STING agonist 22 demonstrated in vivo antitumor effect in an MC38 mice model, with STING pathway activation and production of type I IFNs and proinflammatory cytokines, serum levels of IL-6, G-SCF, and MIP-1β.

Stafia-1 prodrug is the cell‐permeable prodrug of Stafia-1, suitable for cell based assays, inhibits tyrosine phosphorylation of STAT5a with selectivity over STAT5b in cultured human leukemia cells.

ST-115 (ST115) is a potent and specific inhibitor of aminopeptidase P2 (XPNPEP2, APP2) with IC50 of 3.7 nM.ST-115 does not inhibit ACE, neprilysin, or multiple other enzymes, and littile inhibition against Aminopeptidase P1/A/B/N (IC50=600 nM->10 uM).ST-115 can reduce bradykinin degradation, increasing its concentration and protective effects when administered intravenously at the start of reperfusion, reduced damaged area of the heart in a mouse model of myocardial infarction.In a rat model of ischemic stroke, ST-115 reduced functional deficits in a skilled walking test by 60% and reduced brain edema by 51%.ST-115 also reduced brain infarct size by 48% in a major subset of rats with small strokes.

SSCI-1 is a highly potent, selective NaV1.7 inhibitor with IC50 of 27 and 82 nM on human and rhesus Nav1.7 channels, respectively.SSCI-1 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 252 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-1 also exhibits high potency in manual patch clamp experiments (IC50=66/295 nM for huma/rhesus Nav1.7 channels).SSCI-1 does not affect myelinated nerve excitability as measured by TT, SSCI-1 inhibits odorant-induced olfaction in the olfactory bulb of rhesus monkeys, measured by fMRI.SSCI-1 inhibits withdrawal responses to noxious heat in rhesus monkeys.

SS-4 (STAT3 inhibitor SS-4) is a highly selective small molecule inhibitor of STAT3 tyrosine phosphorylation that potently inhibits GBM tumorigenesis in vitro and in vivo.SS-4 strongly and selectively inhibits STAT3 Y-705 phosphorylation in MT330 and LN229 GBM cells and inhibits their proliferation and inducs apoptosis with an IC50 of 100 nM.SS-4 increases the expression of STAT3 repressed genes, while decreasing the expression of STAT3 promoted genes.SS-4 markedly reduces the growth of GBM intracranial tumor xenografts.

SRX3262 is a potent, triple BTK/PI3K/BRD4 inhibitor.

SRX3212 (SRX 3212) is a potent, dual BRD4/PI3Kα inhibitor with IC50 of 3.7 nM (BRD4 BD1) and 32 nM (BRD4 BD2), IC50 of 22 nM for PI3Kα.SRX3212 demonstrated strong anti-cancer activity in cyclinD1 dependent mantle cell lymphoma cell lines (Jeko-1, Mino and Z138), a colon carcinoma cell line (HCT116), a MYCN amplified p53 mutated neuroblastoma cell line (SKNBE2) and a PTEN mutated prostate cancer cell line (PC3), with nanomolar to low micromolar IC50 values.

SRI-41897 is a specific small molecule inhibitor of HIV-1 N-terminal region of NL4-3 Vpu (HIV-1 NL4-3 Vpu) with EC50 of 4.4 uM in the GaLV inhibition assays.SRI-41897 blocks Vpu-mediated modulation of CD4, BST-2/Tetherin and antibody dependent cell-mediated toxicity (ADCC).SRI-41897 rescues CD4 surface expression by 47% on infected TZM-GFP cells, also rescues the expression of CD4 and Tetherin in human peripheral blood mononuclear cells (PBMCs).

SR-302 (SR302) is a potent, selective cell-active dual DDR/p38 inhibitor with IC50 of 23/18/125/196 nM for DDR1/DDR2/p38α/p38β, respectively.

SR1555 is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells; SR1555 is devoid of LXR, FXR, and RORα activity, displaces [3H]T0901317 from the ligand binding domain (LBD) of RORγ with IC50 of 1 uM; represses the expression of RORγ while leading to increased expression of FGF21 and adipoQ in pre-adipocyctes, inhibits activation of hormone-sensitive lipase and increased fatty acid oxidation in obese diabetic mice.

SPH5030 is a selective, potent, and irreversible HER2 mutants inhibitor with IC50 of <1 nM against HER2 D769H, D769Y, V777L and R896C mutants.SPH5030 exhibits high relative HER2 selectivity compared with neratinib and pyrotinib.SPH5030 shows significant in vivo antitumor efficacy in xenograft mouse models, especially in a HER2 mutation A775_G776insYVMA xenograft mouse mode.

SP23 is a STING protein degrader (PROTAC) based on a small-molecule STING inhibitor (C-170) and pomalidomide (a CRBN ligand), shows degradation potency with DC50 of 3.2 uM.SP23 exerted high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model by modulating the STING signaling pathway.

SN-6109 (SN6109) is a small molecule inhibitor RIPK-1 with IC50 of 0.45 uM in radiometric kinase assays.SN-6109 reduced MLKL activation EC50 2.5-11.5 uM under long-term necroptosis execution in murine fibroblast L929 cells, and full protection from ATP depletion and membrane leakage in human and murine cells.SN-6109 decreased p-MLKL/MLKL and p-RIPK3/RIPK3 ratios in mouse liver tissue, showed efficacy in an in vivo model of tissue injury and inflammation driven by RIPK1/3-dependent cell death.