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K 02288

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K 02288 Basic information

Product Name:
K 02288
Synonyms:
  • LM-3151 K02288
  • 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
  • K 02288(K 02288a)
  • K02288;K 02288;K-02288
  • CS-1877
CAS:
1431985-92-0
MF:
C20H20N2O4
MW:
352.38
Product Categories:
  • Inhibitors
Mol File:
1431985-92-0.mol
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K 02288 Chemical Properties

Melting point:
201-203°C
Boiling point:
522.2±50.0 °C(Predicted)
Density 
1.232±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
powder
pka
9.33±0.10(Predicted)
color 
white to beige
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Safety Information

RIDADR 
UN 2811 6.1 / PGIII
HS Code 
2933.39.9200
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K 02288 Usage And Synthesis

Description

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair. K02288 is a 2-aminopyridine-based inhibitor of ALK1 and ALK2 with IC50 values of 1.8 and 1.1 nM, respectively. It is less selective for ALK3, 4, 5, and 6 subtypes and the type II BMP receptor ActRIIA, demonstrating IC50 values of 34.4, 302, 321, 6.4, and 220 nM, respectively. K02288 can prevent BMP4-induced SMAD1/5/8 pathway activation in vitro (IC50 = 100 nM) without affecting TGF-β signaling. Furthermore, at 8-10 μM, K02288 has been used to induce the dorsalization of zebrafish embryos. Through specific inhibition of BMP signaling, this compound can be used to research stem cell biology and disease models of musculoskeletal dysplasia and cancer.

Uses

K02288 is a potent and selective type 1 BMP (bone morphogenetic protein) receptor inhibitor with in vitro activity against ALK-2 (activin receptor-like kinase-2) at low nanomolar concentrations. K02288 also inhibits the BMP-induced Smad pathway without affecting TGF-β signaling and induces dorsalization of zebrafish embryos.

General Description

K02288 is a 2-aminopyridine compound.

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.

storage

Store at -20°C

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.

K 02288Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Email
chenyj@titansci.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
TOKYO CHEMICAL INDUSTRY CO., LTD.
Tel
03-36680489
Email
Sales-JP@TCIchemicals.com
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