kbp

KBP-7018 is a potent and highly selective tyrosine kinase inhibitor that simultaneously targets three key fibrotic-associated kinases, including c-KIT, RET, and PDGFR, with IC50 values of 10 nM, 7.6 nM, and 25 nM respectively, and is therefore widely applicable for mechanistic research into fibrotic signaling pathways, kinase-driven disease progression, and pharmacological intervention strategies aimed at modulating aberrant tyrosine kinase activity.

KBP-7018 Hydrochloride is a novel, tyrosine kinase-selective inhibitor with potent effects on three fibrotic kinases (c-KIT, PDGFR, and RET).

GSK-2793660 is a cathepsin C inhibitor that may be useful in the treatment of cystic fibrosis, noncystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis.

Zifanocycline (KBP-7072) TFA is a semi-synthetic aminomethylcycline antibiotic with oral bioavailability that targets bacterial ribosomes to impede their function. Displaying a broad spectrum of in vitro antimicrobial efficacy, it combats both Gram-positive and Gram-negative bacteria, including numerous multidrug-resistant strains. Clinical investigations focus on treating acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections [1] [2].

Imigliptin (KBP 3853) is a novel dipeptidyl peptidase-4 inhibitor for the study of type 2 diabetes.

Pirotinib is an orally available inhibitor targeting the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, exhibiting potential antineoplastic activity.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.

dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].

PROTAC FKBP Degrader-3 is a bifunctional PROTAC molecule composed of an FKBP ligand-binding group, a rationally designed linker, and a VHL E3 ligase-binding moiety, and functions as a potent FKBP degrader, enabling selective protein degradation studies and validation of FKBP as a therapeutic target.

FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.

FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.

FKBP12 Ligand-Linker Conjugate 2 is a conjugate composed of an FKBP12 target protein ligand and a linker. It is utilized in the synthesis of FKBP12PROTACFM4.

FKBP12PROTACFM4 is a PROTAC degrader targeting MTH1, with a degradation efficiency (Dmax) greater than 90%.

FKBP12 ligand-2 (compound d) is a high-affinity ligand that targets FKBP12. This compound is utilized to selectively enhance the binding of heterobifunctional molecules to BRD4, facilitating the intracellular accumulation of drugs through the "CellTrap" effect. It forms a ternary complex of FKBP12-ligand-BRD4, which inhibits BRD4, suppresses the expression of BRD4 target genes such as MYC, and induces tumor cell death. FKBP12 ligand-2 is applicable in selective cancer research based on the differential levels of presenter proteins within cells.

BRD4/FKBP12 degrader-1 (a1d) is an anticancer agent that functions as a BRD4/FKBP12 degrader.

FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. It is utilized to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching drugs intracellularly through the "CellTrap" effect to form an FKBP12-ligand-BRD4 ternary complex. This complex inhibits BRD4, reducing the expression of BRD4 target genes such as MYC, leading to tumor cell death. FKBP12 ligand-3 can be applied in selective cancer research based on differences in intracellular presenter protein levels.

BRD4/FKBP12 degrader-2 (a1d) is a BRD4/FKBP12 degrader with anticancer activity.

EcDHFR/FKBP12 F36V binder-1 (compound 1) is a bifunctional molecule that integrates the domains of Escherichia coli dihydrofolate reductase (EcDHFR) and FKBP12F36V.

FKBP12-IN-Q2 is an inhibitor of FKBP12.

FKBP51F67V-selective antagonist Ligand2 (example 3-3), a potent ligand, selectively binds to FKBP51 F67V variant without affinity for wild-type FKBP51 or FKBP52 [1], and effectively reverses the anxiogenic phenotype resulting from FKBP51 F67V overexpression in the amygdala.

FKBP51-Hsp90-IN-1 (Compound D10) serves as a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, demonstrating an IC 50 value of 0.1 μM against FKBP51. It holds potential for research applications in stress-related diseases, Alzheimer's disease, and metabolic disorders [1].

FKBP51-Hsp90-IN-2 (Compound E08) functions as a selective inhibitor for the FKBP51 - Hsp90 protein-protein interaction, exhibiting IC 50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. Beyond its inhibitory actions, FKBP51-Hsp90-IN-2 enhances cellular energy metabolism and promotes neurite growth. This compound is utilized in the study of neurodegenerative diseases and cancer [1].