1. TGF-beta/Smad
  2. TGF-β Receptor
  3. LDN-212854

LDN-212854 

Cat. No.: HY-15897 Purity: 99.70%
COA Handling Instructions

LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).

For research use only. We do not sell to patients.

LDN-212854 Chemical Structure

LDN-212854 Chemical Structure

CAS No. : 1432597-26-6

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Solution
10 mM * 1 mL in DMSO USD 134 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 122 In-stock
10 mg USD 226 In-stock
25 mg USD 450 In-stock
50 mg USD 810 In-stock
100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC)[1][2].

IC50 & Target[1]

ACVR1

1.3 nM (IC50)

ALK1

2.4 nM (IC50)

BMPR1A

85.8 nM (IC50)

ALK4

2133 nM (IC50)

ALK5

9276 nM (IC50)

In Vitro

LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2−/− cells[1].
LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells[2].
LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1]
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)[1]
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.
Molecular Weight

406.48

Appearance

Solid

Formula

C25H22N6

CAS No.
SMILES

C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (73.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4601 mL 12.3007 mL 24.6015 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL
10 mM 0.2460 mL 1.2301 mL 2.4601 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.70%

References
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LDN-212854 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LDN-212854
Cat. No.:
HY-15897
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