VU 0364849

Research use only, not for human use.

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

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.

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.

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.

VU 0364849 | DMH2 | DMH 2

TGF-beta/Smad

TGFBR

TGFBR

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1206711-14-9

451.53

C27H25N5O2

>98% (HPLC)

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N1(CCOC2=CC=C(C3=CN4C(N=C3)=C(C5=CC=NC6=CC=CC=C56)C=N4)C=C2)CCOCC1

4-(2-(4-(3-(quinolin-4-yl)pyrazolo[1,5-a]pyrimidin-6-yl)phenoxy)ethyl)morpholine

(-20℃)

With Ice Pack

≥ 2 years