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LDN212854

SKU: orb1226289

Description

LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.

Images & Validation

Key Properties

CAS Number1432597-26-6
MW406.48
Purity>98% (HPLC)
FormulaC25H22N6
SMILESC12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
TargetALK
SolubilityDMSO: 81 mg/mL warmed (199.27 mM)

Bioactivity

In Vivo
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model. Animal model: Murine inducible transgenic ALK2Q207D model of heterotopic ossification. Dosage: 6 mg/kg. Administration: Intraperitoneal injection, twice daily for 4 weeks. Result: Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice. Animal model: HCC xenografts (Huh7 or MT cell). Dosage: 6 mg/kg. Administration: Intraperitoneal injection, twice daily for 10-14 days. Result: Inhibited tumor growth and showed less spheroid/colony formation ability than PBS-treated tumor cells.
In Vitro
LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2-/- cells. LDN-212854 (2.5 μM, 5 days) inhibits cell proliferation in Huh7 and MT cells. LDN-212854 (0.5 μM, 48 h) suppresses ID1 and EpCAM expression in Huh7 and MT cells. Western blot analysis. Cell line: BMPR2-deficient pulmonary vascular smooth muscle cells. Concentration: 0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM. Incubation time: Result: Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

LDN212854 | LDN 212854 | LDN-212854

Similar Products

  • LDN-212854 [orb1307185]

    99.38%

    1432597-26-6

    406.48

    C25H22N6

    10 mg, 25 mg, 1 mg, 5 mg, 50 mg, 100 mg, 200 mg, 1 ml x 10 mM (in DMSO), 2 mg
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LDN212854 (orb1226289)

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