B02

RAD51 Inhibitor B02 (B02) (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.

CCB02 is a selective CPAP-tubulin interaction inhibitor (IC50: 689 nM) with anti-tumor activity, showing no inhibition on cell cycle- and centrosome-related kinases, nor affecting the phosphorylation status of Aurora-A, CDK2, Plk1, Plk2, and CHK1.

ART-CHEM-BB B025267 is the upregulator of utrophin production with EC50 of 1.8 μM and can be used in research on the treatment of Duchenne muscular dystrophy.

B022 is a selective and potent NF-κB-induced kinase (NIK) inhibitor (Ki: 4.2 nM) and a chemical probe for treating liver inflammation and injury, protecting the liver from inflammation and injury caused by oxidative stress and toxins.

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, also known as a molecular glue, that facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, thus forming KB02-SLF[1] and enhancing the longevity of protein degradation in biological systems.

BIIB021 (CNF2024) is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7 nM, EC50=38 nM).

AB023a is an antibiotic with antifungal properties.

AB023b is an antibiotic with antifungal properties.

KB02-COOH is a synthetic fragment derived from ubiquitin E3 ligase ligand KB02, which possesses potential utility in the synthesis of PROTAC compounds. Notably, KB02-COOH can be employed in the generation of PROTAC constructs like KB02-JQ1 and KB02-SLF.

B026 is a selective, orally active inhibitor of p300 CBP histone acetyltransferase (p300 CBP HAT) that acts on p300 (IC50: 1.8 nM) and CBP (IC50: 9.5 nM). b026 exhibits anticancer effects on androgen receptor positive (AR+) prostate cancer cells.

BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2 Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses.

SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.

IMAB027 (ASP1650) is a selective monoclonal antibody against CLDN6 (Claudin 6) with antitumor activity that induces death of CLDN6+ cancer cells through antibody-dependent and complement-dependent cytotoxicity.

Rad51-in-1 is a derivative of B02 and an effective inhibitor of Rad51.