1431985-92-0

Basic information

• Product Name: K 02288
• Synonyms: K 02288;3-[(6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;K 02288 Phenol, 3-[6-amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]-;K02288 3-[(6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;LM-3151 K02288;K 02288(K 02288a);K 02288a
• CAS NO: 1431985-92-0
• Molecular Formula: C20H20N2O4
• Molecular Weight: 352.3838
• Product Categories: Inhibitors
• Mol File: 1431985-92-0.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 522.2±50.0 °C(Predicted)
• Appearance: /
• Density: 1.232±0.06 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 9.33±0.10(Predicted)
• CAS DataBase Reference: K 02288(CAS DataBase Reference)
• NIST Chemistry Reference: K 02288(1431985-92-0)
• EPA Substance Registry System: K 02288(1431985-92-0)

Safety Data

• RIDADR: UN 2811 6.1 / PGIII
• Hazardous Substances Data: 1431985-92-0(Hazardous Substances Data)

Usage

Description

K 02288, also known as a 2-aminopyridine compound, is a potent and selective type 1 bone morphogenetic protein (BMP) receptor inhibitor. It specifically targets activin receptor-like kinases (ALK1-7), which play a crucial role in the assembly of SMAD complexes and the regulation of normal development and tissue repair. K 02288 demonstrates high selectivity for ALK1 and ALK2 with IC50 values of 1.8 and 1.1 nM, respectively, and can inhibit BMP4-induced SMAD1/5/8 pathway activation without affecting TGF-β signaling. Additionally, it has been used to induce the dorsalization of zebrafish embryos at concentrations of 8-10 μM.

Uses

Used in Pharmaceutical Research:
K 02288 is used as a research tool for studying the role of BMP type I receptors in various biological processes, including stem cell biology, tissue repair, and the development of musculoskeletal dysplasia and cancer.
Used in Drug Development:
K 02288 is used as a lead compound in the development of novel therapeutics targeting the BMP signaling pathway, which may have potential applications in the treatment of various diseases and conditions related to abnormal BMP signaling.
Used in Cell Biology:
K 02288 is used as a selective inhibitor of ALK1 and ALK2 to investigate the specific roles of these receptors in cellular processes and to understand the underlying mechanisms of BMP signaling in normal and disease states.
Used in Developmental Biology:
K 02288 is used as a tool to induce dorsalization in zebrafish embryos, providing insights into the role of BMP signaling in embryonic development and pattern formation.
Used in Cancer Research:
K 02288 is used as an inhibitor of the BMP-induced Smad pathway to study its potential role in cancer progression and to explore its therapeutic potential in combination with conventional chemotherapeutic drugs for enhancing chemo-sensitivity and efficacy in resistant cases.

Biochem/physiol Actions

K02288 is functionally similar to dorsomorphin, which is known to be the first small-molecule for BMP signaling inhibition.BMP signalling is associated with many important physiological processes. It acts a central regulator of developmental processes such as organogenesis, gastrulation, mesoderm induction and endochondral bone formation. BMP signals are also related to diseases including pulmonary hypertension, juvenile polyposis syndrome, fibrodysplasia ossificans progressiva and hereditary hemorrhagic telangiectasia syndrome. BMP signaling inhibition might serve as a tool to study its role in other biological processes.

references

[1] sanvitale ce, kerr g, chaikuad a, ramel mc, mohedas ah, reichert s, wang y, triffitt jt, cuny gd, yu pb, hill cs, bullock an. a new class of small molecule inhibitor of bmp signaling. plos one. 2013 apr 30;8(4):e62721.