Enzymes

PTPN2/1-IN-2 is a PTPN2/1 antagonist that can be used in various tumor research.

PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer.

LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress.

MMP-7-IN-3 is a potent and selective inhibitor of MMP-7.

MMP-9/10-IN-2 (compound 6e) is a potent inhibitor of MMP10 and MMP9, with IC50 of 0.076 μM for MMP10, and 93.18% inhibition at 0.5 μM for MMP9.

BPU arrests cell cycle progression in the sub-G1 phase.

(R)-Azasetron besylate (SENS-401) is an orally active calcineurin inhibitor.

Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 is a fluorescently quenched peptide substrate that can be used to detect the activity of matrix metalloproteinases (MMPs) and their associated tumor necrosis factor converting enzyme (TACE) (Ex/Em=325nm/400nm).

AV5116 is a cap-dependent endonuclease inhibitor ( CENI ) that binds to the active site of the cap-dependent endonuclease (CEN) located in the N-terminal domain of the polymerase acidic.

Cusculine (FAC21) is an oropouche virus (OROV) endonuclease inhibitor with an IC 50 of 1.4 μM.

Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail - CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis [1] .

BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS ), non-covalent pan- KRAS inhibitor ( IC 50 =28-120 nM).

RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form).

CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor ( CCKBR ) agonist with an EC 50 of 35 pM.

ZX-J-19L is a CyPJ inhibitor with inhibitory activity against a variety of tumor cell lines.

DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor ( IC 50 =0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 ( IC 50 values are 1.1 nM and 73 nM, respectively).

KVD-001 is a potent plasma kallikrein inhibitor.

IL13Rα2 D1 is an effective IL-13/IL13Rα2 signaling axis inhibitor.

PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor ( IC 50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels.

PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC 50 of 0.16 μM.

Royleanonic acid is an abietan-type diterpene found in the leaves of Salvia officinalis L.

LacCer (d18:1/20:0) is a lipid whose level is closely associated with atherosclerosis and cardiovascular diseases [1] .

MMP-9-IN-13 (Example 1) is a selective inhibitor of human MMP9 with an IC 50 value of 0.02 nM.

C-telopeptide acetate is a cross-linked peptide of type I collagen that is released during bone resorption and correlates with bone mineral density (BMD).