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Chemical Structure| 1432597-26-6 Chemical Structure| 1432597-26-6

Structure of LDN-212854
CAS No.: 1432597-26-6

Chemical Structure| 1432597-26-6

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LDN-212854 is an inhibitor of BMP and can inhibit ALK2 with IC50 of 1.3 nM. It is used to prevent heterotopic ossification.

Synonyms: BMP Inhibitor III

4.5 *For Research Use Only !

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Product Details of LDN-212854

CAS No. :1432597-26-6
Formula : C25H22N6
M.W : 406.48
SMILES Code : C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
Synonyms :
BMP Inhibitor III
MDL No. :MFCD28099808
InChI Key :BBDGBGOVJPEFBT-UHFFFAOYSA-N
Pubchem ID :60182388

Safety of LDN-212854

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • ALK1

    ALK1, IC50:2.4 nM

  • TGFβRI/ALK5

    ALK5, IC50:9276 nM

  • ALK2

    ALK2, IC50:1.3 nM

  • ALK3

    ALK3, IC50:85.8 nM

  • ALK4

    ALK4, IC50:2133 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Mesenchymal cells 750 nM 12, 24, 48, 72, and 96 hr Evaluate the effect of LDN-212854 on mesenchymal cell proliferation, results show LDN-212854 significantly reduces cell proliferation Mol Ther. 2017 Aug 2;25(8):1974-1987.
Bone marrow mononuclear cells (BMMs) 1 μM 5 days LDN-212854 inhibits SMAD1/5/9 phosphorylation, thereby inhibiting osteoclastogenesis in caAcvr1 mutant cells. J Biol Chem. 2019 Nov 22;294(47):17818-17836.
Primary rat OPCs 0.18 μM 3 days To evaluate the effect of LDN-212854 on OPC differentiation in the presence of fibrinogen, results showed that LDN-212854 restored mature oligodendrocyte differentiation and reduced GFAP+ astrocyte formation. Brain. 2021 Sep 4;144(8):2291-2301.
HSG cells 0.1, 1.0 or 10 nM 4 days To investigate the effect of LDN-212854 on BMP6-induced loss of cell membrane water permeability. Results showed that LDN-212854 inhibited BMP6-induced RVD loss in a dose-dependent manner. Sci Rep. 2020 Feb 19;10(1):2967.
HSG cells 10 or 60 nM 24 hours To investigate the effect of LDN-212854 on BMP6-induced SMAD1/5/8 phosphorylation. Results showed that 60 nM LDN-212854 significantly reduced BMP6-induced SMAD1/5/8 phosphorylation. Sci Rep. 2020 Feb 19;10(1):2967.
C2C12 cells 500 nM 3 days To test the inhibitory effect of LDN-212854 on BMP2-induced alkaline phosphatase (ALP) activity, results showed that LDN-212854 significantly suppressed ALP activity. Stem Cell Res Ther. 2024 Apr 5;15(1):98.
Human mesenchymal stromal cells (MSCs) 500 nM 28 days To test the effect of LDN-212854 on MSC chondrogenesis in vitro, results showed that LDN-212854 mildly inhibited chondrogenesis but had limited effects on hypertrophy markers. Stem Cell Res Ther. 2024 Apr 5;15(1):98.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Ntv-a;p53fl/fl mice Intraperitoneally 6 mg/kg Twice daily for 5 consecutive days (in vitro); twice a day until euthanasia endpoints were met (in vivo survival study) To evaluate the effect of LDN212854 on tumor growth and survival, results showed that LDN212854 significantly prolonged survival. Nat Commun. 2019 Mar 4;10(1):1023.
Mice Burn/tenotomy model Intraperitoneal injection 6 mg/kg Daily for 6 weeks Evaluate the effect of LDN-212854 on trauma-induced heterotopic ossification, results show LDN-212854 significantly reduces heterotopic ossification volume Mol Ther. 2017 Aug 2;25(8):1974-1987.
Mouse Acvr1[R206H]FlEx/+ conditional knock-in mice Subcutaneous injection 3 mg/kg Twice daily for 4 weeks LDN-212854 effectively suppressed spontaneous joint/ligament HO and injury-triggered intramuscular HO in Acvr1R206H mice, demonstrating selective ACVR1 inhibition abrogates cell-autonomous effects of mutant receptors in tendon and muscle progenitors. Sci Transl Med. 2016 Nov 23;8(366):366ra163
Mice C57BL/6.NOD-Aec1Aec2 mouse model Intraperitoneal injection 2.5 mg/kg Once daily for 24 days To investigate the effect of LDN-212854 on the restoration of salivary gland function in C57BL/6.NOD-Aec1Aec2 mice. Results showed that LDN-212854 treatment significantly increased salivary flow rate and reduced phosphorylation of SMAD1/5/8 and expression of ID3. Sci Rep. 2020 Feb 19;10(1):2967.
NCG mice HCC xenograft model Intraperitoneal injection 6 mg/kg Twice daily for 10-14 days LDN-212854 significantly suppressed HCC tumor growth and induced global RNA m6A methylation Int J Mol Sci. 2024 Jan 12;25(2):981.
NOD/SCID mice HCC xenograft model Intraperitoneal injection 6 mg/kg Twice daily for 10-14 days Inhibited HCC tumor growth and angiogenesis Int J Mol Sci. 2022 Jan 27;23(3):1475.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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