PDM 11 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

PF 3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 uM).

Pirozadil is a hypolipidemic agent.

PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding.

PXS-5153A (PXS5153A) is a potent, selective, fast-acting, dual LOXL2/LOXL3 inhibitor with IC50 of <40 nM against all mammalian species LOXL2, inhibits human LOXL3 with IC50 of 63 nM.

SRI-011381 is an agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.

Sulfaphenazole is an inhibitor of CYP2C9 (Ki = 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Kis = 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases.

PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.

PIK-75 is a selective cell-permeable inhibitor of PI 3-kinase p110α (IC50 values are 5.8, 76 nM and 1.3 μM at PI 3-kinase p110α, PI 3-kinase p110γ and PI 3-kinase p110β respectively). Inhibits production of PIP2 and PIP3 in adipocytes, phosphorylation of

YX-I-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically inhibits amyloid formation; YX-I-1 inhibits the aggregation of wt hIAPP, extending the t50 from 15.1 ± 0.2 h to 23.4 ± 1.0 h at a 1:7 molar ratio of peptide:inhibitor. YX-I-1 inhibits primary nucleation, secondary nucleation and elongation of wt hIAP. YX-A-1 is a useful chemical tools to study hIAPP aggregation.

YX-A-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically enhances amyloid formation; YX-A-1 accelerates wt hIAPP assembly, even when added in substoichiometric concentration ratios (e.g. at a peptide:YX-A-1 molar ratio of 1:0.5 the t50 is reduced ~1.5-fold). YX-A-1 is a useful chemical tools to study hIAPP aggregation.

YX-2-115 is a palbociclib derivative compound with piperazine-linker tail for PROTAC YX-2-107 synthesis, inhibits CDK6 with IC50 of 4.5 nM.

YTK-105 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YTK-105 for AUTOTAC design.

YTK-105 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.

YOK-2204 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YOK-2204 for AUTOTAC design.

YOK-2204 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.

YOK-1304 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.AUTOphagy-TArgeting Chimera (AUTOTAC) is a general chemical tool and platform technology, which employs bifunctional molecules composed of target-binding ligands linked to autophagy-targeting ligands.AUTOTACs bind the ZZ domain of the otherwise dormant autophagy receptor p62/Sequestosome-1/SQSTM1, which is activated into oligomeric bodies in complex with targets for their sequestration and degradation.

YOK-1304 AUTOTAC intermidate 1 is an intermidate for AUTOTAC design.

Wbox2 is a membrane-permeant peptide that potently inhibits clathrin-mediated endocytosis (CME, IC50=3 uM), binds to SNX9 and AP2 and perturbs clathrin interactions with AP2 and SNX9.Wbox2 has no effect on cell viability at ≤30 uM and exhibited an IC50 for cytotoxicity (>40 uM) that is 10-fold higher than that needed to inhibit CME.Wbox2 interferes with AP2–clathrin interactions and alters CCP dynamics, binds to both AP2 and SNX9 with binding affinities of 4.0 and 26.2 uM.

TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.

Thailanstatin D (TST-D) is a potent antiproliferative natural product and direct precursor of Thailanstatin A, inhibits eukaryotic RNA splicing with stiong anti-tumor activities.Thailanstatin D inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and Thailanstatin D preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site.Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis.Thailanstatins are attractive cytotoxin agent for ADC design.

Thailanstatin B is a potent antiproliferative natural product and pre-mRNA splicing inhibitor, potential antibody-drug conjugate payload.

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

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.

SHP2 PROTAC R1-5C is a potent and highly selective SHP2 PROTAC created by conjugating RMC-4550 with pomalidomide using a PEG linker, with a low nanomolar DC50; SHP2 PROTAC R1-5C is highly selective for SHP2, induces degradation of SHP2 in leukemic cells at submicromolar concentrations. SHP2 PROTAC R1-5C inhibits MAPK signaling, and suppresses cancer cell growth. SHP2 PROTACs serve as an alternative strategy for targeting ERK-dependent cancers and are useful tools alongside allosteric inhibitors for dissecting the mechanisms by which SHP2 exerts its oncogenic activity.

MS910 (MS-910) is the first CRBN-recruiting MEK1/2 degrader (PROTC) with HT29 DC50 of 118/55 nM for MEK1/2 degradation, respectively.MS910 displays antiproliferation potency against HT29 cell with GI50 of 330 nM, degrade MEK1 and MEK2 and inhibit pERK signaling in a time-dependent manner.

LCC03 is a salicylanilide derivative and autophagy inducer, dose-dependently suppresses proliferation and retarded cell-cycle progression in CRPC cells (IC50, 0.69 to 4.8 uM).The classical autophagy features, including autophagosome formation and LC3-II conversion, were dramatically shown in LCC03-treated CRPC cells, which was associated with the suppressed AKT/mTOR signaling pathways, a major negative regulator of autophagy.LCC03 also showed an expanded morphology of the endoplasmic reticulum (ER), increased expression of the ER stress markers GRP78 and PERK, and eIF2α phosphorylation.The PERK-eIF2α pathway contributed to the LCC03-induced autophagy.LCC03 suppressed the growth of CRPC xenografts in mouse bone without systemic toxicity in tumor-bearing mice.

K-312 is a novel cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 60 nM, also suppresses hepatocyte expression of PCSK9, raises HDL and lowers LDL cholesterol levels in vivo; raises HDL cholesterol, decreases LDL cholesterol, and attenuates aortic atherosclerosis in cholesterol-fed rabbits; decreases PCSK9 expression in human primary hepatocytes and in the human hepatoma cell line HepG2, decreases the occupancy of SREBP-1 and SREBP-2 on the sterol regulatory element of the PCSK9 promoter.

HDAC8 PROTAC 1 is a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8).HDAC8 PROTAC 1 induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.