Inhibitors

Tauro-obeticholic acid, a farnesoid X receptor (FXR) agonist and semisynthetic derivative of chenodeoxycholic acid, is an active metabolite of obeticholic acid.

Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive

Compound B12 (Antibacterial agent 157) is a fungicidal agent that can impact protein synthesis in Botrytis cinerea.

RIOK2-IN-2 (8) functions as an inhibitor of RIOK2, exhibiting IC50 values of 3.02 μM in MKN-1 cells and 5.34 μM in MOLT4 cells [1].

Sakura 6, a synthetic serotonin transporter (SERT)-binding peptide, enhances the interaction between SERT and neuronal nitric oxide synthase.

Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].

Mal-VC-PAB-PNP-CDN-A is a conjugate comprised of an agent and a linker, utilized in antibody-drug conjugates (ADC) [1] [2].

VISTA-IN-2 (Compound 1) is a V-domain Ig suppressor of T-cell activation (VISTA) inhibitor that promotes the degradation of VISTA in cells via autophagy,

Py-MAA-Val-Cit-PAB-MMAE (AAJ8D6-PY-Val-Cit-MMAE) serves as an ADC linker for Zapadcine-3a, a broad-spectrum anti-TRAILR2 ADC with antineoplastic properties.

Davelizomib is a proteasome inhibitor that exhibits antineoplastic activity [1].

EST73502 is a compound that functions as a dual agonist for the μ-opioid receptor (MOR) and an antagonist for the σ1 receptor (σ1R). It is selective, orally active, and possesses the ability to penetrate the blood-brain barrier (BBB). The compound exhibits a Ki value of 64 nM for the MOR and 118 nM for the σ1R. Additionally, EST73502 demonstrates antinociceptive activity [1].

(αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, serves as a cytotoxic agent that effectively inhibits the proliferation of U87MG

HBV-IN-38 (Example 193), an HBV DNA inhibitor with an EC50 value of ≤100 nM, serves as a research tool for investigating viral infections [1].

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].

ATR-IN-24 (Compound 1) is an ATR inhibitor with demonstrated anticancer activity [1].

Compound 11, also known as Antitumor Photosensitizer-2, is a potent photosensitizer with remarkable photodynamic anti-tumor properties and minimal skin photo-

FAP-IN-2 is a 99mTc-labeled, isonitrile-containing derivative of a fibroblast activation protein (FAPI) inhibitor suitable for tumor imaging [1].

PHI-101 is a checkpoint kinase 2 (Chk2) inhibitor that can be used for the study of refractory acute myeloid leukemia (AML) and ovarian cancer.

hDHODH-IN-8 is a potent human dihydroorotic dehydrogenase (hDHODH) inhibitor (IC50: 16 nM) that exhibits potent antiproliferative effects and has good water solubility, with potential for oncology studies, especially in lymphoma.

Ifetroban sodium (BMS-180291), oral TXA2/PGH2 antagonist for researching heart, stroke, BP, thrombosis.

BPH-628 is a bioactive chemical.

ROCK-IN-6, a selective ROCK2 inhibitor, exhibits potent inhibition with an IC50 of 2.19 nM and holds promise for research into glaucoma and retinal diseases [1

Ifetroban is a potent and selective TxA2/PGH2 receptor antagonist.