Enzymes

PTPN2/1-IN-2はPTPN 2/1アンタゴニストであり、様々な腫瘍研究に使用できる。

PP5-IN-1(化合物p053)は、セリン/スレオニンプロテインホスファターゼ5 (pp5)の競合的阻害剤であり、その触媒ドメインに結合して腎がんのアポトーシスを引き起こす。

LYP-IN-3選別(複合D34)は剤うとLymphoid-tyrosineホスファターゼ(LYP)(紀= 0.93μM)シグナリング経路ドーパミン受容体調整とピン受容体(TCR)進んで腫瘍ます

MMP-7-IN-3はMMP-7の強力な選択的阻害剤である。

MMP-9/10-IN-2（化合物6 e）はMMP 10とMMP 9の強力な抑制剤であり、MMP 10に対するIC 50は0.076μM、MMP 9に対するIC 50は0.5μMの場合の抑制率は93.18%である。

BPU細胞周期プロセスをサブG 1期にブロックする。

(R)-Azasetron besylateSENS-401は経口活性カルシウム変性ニューリン酸酵素阻害剤である。

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).