pb1

PB1 is a highly-effective intracellular disulfide reducing agent with notable attributes such as excellent cell permeability, the capacity to generate a substantial intracellular concentration gradient, and remarkable stability. It serves as a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 demonstrates the potential to enhance the survival of retinal ganglion cells following axotomy in vitro at concentrations in the nanomolar and picomolar range. Consequently, PB1 has proven instrumental in the study of neuroprotective properties[1][2][3].

3-Phenylbutyric acid undergoes metabolism through initial oxidation processes involving both its benzene ring and side chain. It serves as an effective agent for the isolation of Rhodococcus rhodochrous PB1 from compost soil.

SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2, SMARCA4, PB1(2), PB1(3), and PB1(5) with Kds of 35 nM, 36 nM, 3.7 μM, 2.0 μM, and 13 nM, respectively.

PFI-3 is a selective chemical inhibitor for SMARCA (2/4) (Kd = 89 nM)and PBI (5) bromodomains which may result in the delay and prevention of breast cancer.

PB17-026-01 is an effective allosteric inhibitor of SHP2, exhibiting its highest inhibitory activity with an IC50 of 38.9 nM. PB17-026-01 is applicable to cancer research.

TPB15 is an orally active inhibitor of Hh (Hedgehog) signalling. TPB15 significantly blocks the MDA-MB-468 cell cycle and induces apoptosis. TPB15 blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. TPB15 has good anti-tumour effects and low toxicity.

PB118 has the capacity to effectively clear Aβ deposits by augmenting phagocytosis, enhance the tubulin/microtubule network through increased acetyl α-tubulin levels, modulate various inflammation-associated cytokines and chemokines, and notably diminish phospho-tau (p-tau) levels linked to Alzheimer's disease (AD). The IC50 of PB118 for HDAC6 is 5.6 nM.

PB131, a selective and brain-permeable HDAC6 inhibitor, exhibits high binding affinity (IC50: 1.8 nM) and potent anti-inflammatory activity, making it suitable for inflammation research, particularly in neuroinflammation [1].

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

OPB-111077 is an inhibitor of one or more signal transducers and activators of transcription (STAT) proteins.

OPB-171775 is a molecular glue that forms a ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces cell death mediated by SLFN12 RNase, activates the SLFN12 RNase-associated GCN2 signaling pathway, and demonstrates antitumor activity.

PBT-1033 (PBT-2) is a potential neuroprotective agent for the treatment of Alzheimer's disease and Huntington's disease.

PB-119 is a PEGylated exenatide that lowers blood glucose levels by enhancing β cell function and reducing insulin resistance. It is applicable in studies related to type 2 diabetes.

NSC 80538 is an inhibitor of MEK Kinase PB1 Domains in multiplex HTS assays.

Bromodomain Inhibitor-13 (Compound 1), an analog of PFI-3, is a bromodomain-containing protein (BCP) inhibitor. It specifically targets the bromodomains of SMARCA2, SMARCA4, and the first and second bromodomains of PB1 [PB1(5) and PB1(2)], with dissociation constants (KD) of 37, 53, 30, and 190 nM, respectively.

RdRP-IN-8 (compound 45) is an antiviral agent targeting influenza viruses. It inhibits the viral RNA-dependent RNA polymerase (RdRP) activity by disrupting the heterodimerization of the PA and PB1 subunits, with an IC50 value of 0.13 μM.

SGC-BRDVIII-NC (Compound 35) serves as a negative control for the SMARCA2/4 and PB1 bromodomain (BRD) inhibitors. The binding ability of the protein-ligand is completely eliminated in SGC-BRDVIII-NC through the methylation of the phenolic hydroxyl group. This compound is applicable for research in adipogenesis.

Anti-Influenza agent 10 (Compound 41) is an inhibitor of the RNA-dependent RNA polymerase (RdRp) of the influenza A virus. It shows potent antiviral activity against the A/PR/8/34(H1N1) strain, with an IC50 of 0.29 μM and a KD of 4.11 μM. The compound functions by disrupting the interaction between the PA and PB1 subunits, inhibiting the assembly of the viral RdRp complex, and thereby blocking transcription and replication of the viral genome. Anti-Influenza agent 10 also demonstrates significant broad-spectrum efficacy against various influenza strains, such as H3N2, H3N8, and H9N2, with IC50 values of 3.96, 1.91, and 1.45 μM, respectively. It is useful for research on influenza A virus infections.

Jegosapogenol A is a type of triterpenoid. Triterpenoids are terpene molecules containing six isoprene units. Barringtogenol C is a very weakly acidic compound (based on its pKa) and practically insoluble (in water). Barringtogenol C exists in tea. It can

RdRP-IN-4 (compound 11q) is an arylbenzohydrazide analogue, an orally active inhibitor of influenza A virus RNA-dependent RNA polymerase (RdRp) that directly binds the PB1 subunit of RdRp. RdRP-IN-4 inhibited H1N1 (A/PR/8/34) Flu A and Flu B strains (B/Lee/1940) in a dose-dependent manner with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 had a significant antiviral effect in infected mice.

SMARCA2-IN-4 (Compound 26) is an inhibitor of the SWI/SNF chromatin remodeling complex SMARCA, specifically targeting its bromodomain. This compound exhibits high affinity for PB1(5), SMARCA2B, and SMARCA4, with dissociation constants (Kd) of 124, 262, and 417 nM, respectively.