VU 0364849

CAS No. 1206711-14-9

VU 0364849( VU 0364849 | DMH2 | DMH 2 )

Catalog No. M10756 CAS No. 1206711-14-9

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    VU 0364849
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM.
  • Description
    A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM; also inhibits ALK6 (Ki<1 nM) and ALK2 (Ki=42.77 nM), little to no affinity for ALK4/5, BMPR2, AMPK etc.; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.
  • In Vitro
    DMH2 decreases expression of Id1 and Id3 and causes growth suppression of three lung cancer cell lines with K-Ras mutation (A549, H157, H727) and three without a K-Ras mutation (H1299, H865, U1752).The combination of DMH2 and PP2 causes significantly greater reduction in Id1 promoter activity and growth inhibition than either agent alone in the A549 cells.
  • In Vivo
    DMH2 (0-2 mg/kg, IP, twice daily, for 2 days prior to PH (partial hepatectomy) and for 2 days after PH) increases hepatocyte proliferation from 13.7% to 26.9% at 2 mg/kg. Animal Model:C57BL/6 mice (7-8 weeks, male)Dosage:0.5, 1, 2 mg/kg Administration:IP, twice daily, for 2 days prior to PH and for 2 days after PH (partial hepatectomy)Result:Increased hepatocyte proliferation from 13.7% to 26.9% at 2 mg/kg.
  • Synonyms
    VU 0364849 | DMH2 | DMH 2
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    TGFBR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1206711-14-9
  • Formula Weight
    451.53
  • Molecular Formula
    C27H25N5O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    N1(CCOC2=CC=C(C3=CN4C(N=C3)=C(C5=CC=NC6=CC=CC=C56)C=N4)C=C2)CCOCC1
  • Chemical Name
    4-(2-(4-(3-(quinolin-4-yl)pyrazolo[1,5-a]pyrimidin-6-yl)phenoxy)ethyl)morpholine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Tsugawa D, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):549-58. 2. Langenfeld E, et al. Mol Cancer. 2013 Oct 26;12(1):129. 3. Langenfeld E, et al. PLoS One. 2013 Apr 12;8(4):e61256.
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