T8807

Benzydamine is a benzyl-indazole having analgesic, antipyretic, and anti-inflammatory effects. Benzydamine is used to reduce post-surgical and post-traumatic pain and edema and to promote healing.

STAT6-IN-5 (example 84) is an inhibitor of STAT6 (IC50 = 0.24 μM), applicable for investigating inflammation and allergies such as atopic dermatitis.

TNG348 is an allosteric, selective, and reversible inhibitor of USP1, causing dose-dependent accumulation of ubiquitinated substrates in vitro and in vivo. CRISPR screens demonstrate that TNG348 disrupts DNA damage tolerance by interfering with the translesion synthesis pathway via RAD18-dependent ubiquitinated PCNA. Although both TNG348 and PARP inhibitors selectively kill homologous recombination-deficient tumors, they act through distinct mechanisms: PARP1 knockout confers resistance to PARP inhibitors but sensitizes cells to TNG348. Consistent with this mechanistic divergence, combining TNG348 with PARP inhibitors results in synergistic antitumor efficacy, including tumor growth inhibition and regression in multiple HRD mouse xenograft models.

CDK4/6-IN-19 (Compound II-7) serves as an inhibitor of CDK4 and CDK6, exhibiting IC 50 values of 0.2 nM and 5.0 nM, respectively. Additionally, it suppresses cell proliferation and is applicable in cancer research.

PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader targeting the epidermal growth factor receptor (EGFR), with a DC50 of less than 100 nM. It binds to CRBN-DDB1 with a Ki of 36 nM. This compound effectively degrades EGFR, focal adhesion kinase (FAK), and RSK1, and inhibits the proliferation of BaF3 wild-type and EGFR mutant cells, exhibiting an IC50 of less than 100 nM.

Compound 11b, known as P-selectin antagonist 1, serves as an antagonist for both pan-selectin, with an IC50 of 82 μM, and E-selectin, with a KD of 0.91 μM.