b 02

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

Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815

EAPB 02303 is a microtubule-disrupting agent and inhibitor that induces mitosis arrest and spindle assembly impairment, leading to apoptosis (programed cell death) and demonstrating antitumor activity. Furthermore, it exhibits potent synergy with Paclitaxel at lower concentrations [1].

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

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.

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.

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

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.

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.

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.

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

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.

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.

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.

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.

BIIB021 (CNF2024) mesylate is the mesylate salt form of BIIB021. BIIB021 is an orally active Hsp90 inhibitor. It suppresses the proliferation of drug-resistant chronic myeloid leukemia (CML) cells, with IC50 values for K562, K562/G, 32Dp210, and 32Dp210-T315I cells recorded at 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 induces the degradation of BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. Furthermore, BIIB021 can induce autophagy in CML cells and is applicable for CML research.

SYY-B029-2 is a potent inhibitor of histone acetyltransferase (HAT) with an IC50 of 1.4 nM. It effectively inhibits the growth of human mantle cell lymphoma (MCL) cell line MAVER-1 and the human castration-resistant prostate cancer cell line LNCaP clone FGC, with IC50 values of 15 nM and 13 nM, respectively.

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

Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1/JAK2 inhibitor.

IDO5L (INCB024360 analogue) is an effective IDO1 inhibitor(IC50=10 nM).