PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

UNC0737 is a negative control of UNC0638 and the N-methyl analog of UNC0638. UNC0737 was designed to eliminate the hydrogen bond interaction seen in the G9a-UNC0224 cocrystal structure between Asp1083 of G9a and the secondary amino group at the 4-position of UNC0224's quinazoline ring3. UNC0737 was >300-fold less potent than UNC0638 in G9a and GLP biochemical assays. As expected, UNC0737 was a poor inhibitor of G9a (IC50 = 5,000 ± 200 nM (n = 2)) and GLP (IC50 > 10,000 nM (n = 2)) in the SAHH-coupled assays.

A novel protein kinase affinity probe...

SN38 NHS ester is the NHS ester derivative of SN38. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis. SN38 NHS ester can be used for the synthesis of antibody-drug conjugates (ADCs).

IT 901 is a c-Rel inhibitor (IC50 = 3 μM). Inhibits IL-2 expression in activated T-cells in vitro.

CBPD-409 is a highly potent, selective and orally bioavailable PROTAC degrader of CBP/p300. CBPD-409 induces robust CBP/p300 degradation with DC50 0.2-0.4 nM and displays strong antiproliferative effects with IC50 1.2-2.0 nM in the VCaP, LNCaP, and 22Rvl AR+ prostatcancer cell lines.

ERAS-0015 is a pan-RAS modulator glue and demonstrates siganificantly more potent inhibition of cellular proliferation across KRAS mutant cell lines vs RMC-6236.

BRD-810 is a potent and selective MCL1 inhibitor with Kd of 0.3 nM (SPR) and IC50 of 0.4 nM (MCL1-Noxa HTRF), respectively. BRD-810 is a rapidly cleared inhibitor of MCL1 that has robust antitumor efficacy in hematological and solid tumor cancer models.

PF-06648671 is a potent γ-secretase modulator with IC50 of 8.9 nM against Aβ42. PF-06648671 has favorable brain availability in rodent, which translated into excellent central exposure in human and robust reduction of amyloid β (Aβ) 42 in cerebrospinal fluid (CSF).

Compound 33 (HYOU1 inhibitor) is a first-in-class inhibitor of hypoxia up-regulated protein 1 (HYOU1) with EC50 of 3.2 μM/2.6 μM/16.1 μM/3.0 μM in WT-MIP3/WT-RANTES/hTNFtg-MIP3/hTNFtg-RANTES, respectively.

Maraviroc (Selzentry, UK-427857, Celsentri) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

CHF-6523 is an inhaled PI3Kδ inhibitor.

AZD4144 is an NLRP3 inhibitor.

BAY-2925976 is an ARα2C antagonist.

BMS-986408 is a DGK inhibitor.

Casdatifanum is a hypoxia-inducible factor (HIF) inhibitor.

GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

CD-005 is a low-molecular-weight gelator that can be used to prepare gels for proteins and vaccines. CD-005 can physically entrap proteins, preventing their irreversible aggregation, and maintain protein function for at least 4 weeks even at temperatures up to 50°C.

TYRA-300 is the first oral selective FGFR3 inhibitor with IC50 of 11 nM in Ba/F3 cells, and shows selectivity over FGFR1, FGFR2 and FGFR4 in Ba/F3 cells was 25-, 14-, and 36-fold, respectively. TYRA-300 demonstrates equivalent potency for FGFR3 WT and V555M/L gatekeeper mutations in enzymatic assays and in engineered RT112/84 and UM-UC-14 bladder cancer cell lines containing the V555M mutation.

AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.

(S,R)-LSN3318839 is the stereoisomer of LSN3318839 (HY-142162). LSN3318839 is an orally active positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.

GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.