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.

AKOS B029051, with CAS No. 2221-13-8, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. AKOS B029051 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

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.

FCOB02 is a monoamine oxidase B (MAO-B) ligand. It can be labeled as [18F]FCOB02, serving as a 4-methylcoumarin-like targeting probe. [18F]FCOB02 demonstrates high affinity for MAO-B, with an IC50 of 10.68 nM. It is utilized for specific imaging and quantitative analysis of MAO-B in vivo.

(2S)-SB02024 (SB02877) is the S-enantiomer of SB02024 and acts as a Vps34 inhibitor.

KB02-amide-PEG2-C2-acid is a synthetic E3 ligase ligand-linker conjugate (E3 ligase Ligand-linker conjugate) commonly used for the synthesis of PROTACs, such as KB02-SLF.

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.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Gimsilumab (MORAb-022) is a humanized monoclonal antibody targeting granulocyte macrophage colony-stimulating factor for the study of COVID-19-induced inflammation and hypoxemia.

Alisporivir (Debio-025) is a cyclophilin A inhibitor that disrupts the interaction between CypA and NS5A. It exhibits anti-hepatitis C virus (HCV) activity in vivo and in vitro, inhibits the replication of MERS and SARS coronaviruses, and promotes antigen-specific CD8(+) T cell activation.

EAPB-0202, the demethylated metabolite of EAPB0203, demonstrates significant in vitro activity against A375 cells when compared to the reference drugs fotemustine and imiquimod.

OSUAB-0284 is an inhibitor of bacterial topoisomerase. It exhibits significant activity against staphylococci, particularly methicillin-resistant Staphylococcus aureus (MRSA). The compound exerts its antibacterial effect by inhibiting bacterial topoisomerase and may be used in research on infections caused by drug-resistant bacteria, including MRSA.

DOTA-ALB-02 is a ligand that binds with albumin and acts as an FAP inhibitor (FAPI). When labeled with 177Lu, DOTA-ALB-02 demonstrates high affinity for FAP, enhancing tumor uptake and retention, and it has a significant tumor-to-nontarget ratio. It is used in PET/CT and SPECT/CT imaging for detecting cancer, particularly advanced stages.