ChemicalBook > CAS DataBase List > LDN212854

LDN212854

Description In vitro In vivo

Product Name: LDN212854
CAS No.: 1432597-26-6
Chemical Name: LDN212854
Synonyms: CS-1202;LDN212854;BMP Inhibitor III;LDN-212854, >=98%;LDN-212854 ，S7147;LDN212854 USP/EP/BP;BMP INHIBITOR III;LDN212854;LDN 212854;LDN-212854 (This product is only available in Japan.);5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyriMidin-3-yl]quinoline;5-[6-[4-(Piperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
CBNumber: CB12684548
Molecular Formula: C25H22N6
Formula Weight: 406.48
MOL File: 1432597-26-6.mol

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LDN212854 Property

Density: 1.33±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: soluble1mg/mL, clear (warmed)
form: powder
pka: 8.79±0.10(Predicted)
color: white to beige
InChIKey: BBDGBGOVJPEFBT-UHFFFAOYSA-N
CAS DataBase Reference: 1432597-26-6

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Safety

Hazard Codes: Xn
Risk Statements: 22
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger
Hazard statements: H301Toxic if swalloed
Precautionary statements: P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0965
Product name: LDN-212854
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $174.8
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML0965
Product name: LDN-212854
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $736
Updated: 2025/07/31

TCI Chemical

Product number: L0347
Product name: LDN-212854
Packaging: 5MG
Price: $128
Updated: 2025/07/31

TCI Chemical

Product number: L0347
Product name: LDN-212854
Packaging: 25MG
Price: $384
Updated: 2025/07/31

Cayman Chemical

Product number: 17698
Product name: LDN-212854
Purity: ≥98%
Packaging: 1mg
Price: $36
Updated: 2024/03/01

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LDN212854 Chemical Properties,Usage,Production

Description

LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.

In vitro

In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6-versus BMP4-induced osteogenic differentiation.

In vivo

LDN-212854 (6 mg/kg, i.p.) effectively neutralize ALK2 signaling in vivo, and potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva.

Uses

5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline, contains the pyrazolo[1,5-a]pyrimidine scaffold, acting as a novel and selective bone morphogenetic protein receptor (BMP) inhibitors. It is a COVID19-related research product.

Biological Activity

ldn-212854 is a selective inhibitor of bone morphogenetic protein (bmp) signaling with ic50 value of 1.2nm [1].in the kinase assay, ldn-212854 shows inhibitory activities against caalk2 and caalk5 with ic50 values of 16nm and 2μm, respectively. it demonstrates that ldn-212854 is selective against bmp over tgf-β signaling. besides that, the inhibition of caalk2 caused by ldn-212854 is 6- and 10-fold more potent than that of caalk1 and caalk3, respectively. in c2c12 cells transfected with bmp receptors, ldn-212854 also exerts preferential inhibition against caalk2. furthermore, in a transgenic alk2q207d model of heterotopic ossification, treatment of ldn-212854 prevents the formation of heterotopic bone and preserves limb range of motion [1].

Biochem/physiol Actions

LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2).

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].

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.

IC 50

ACVR1: 1.3 nM (IC₅₀); ALK1: 2.4 nM (IC₅₀); BMPR1A: 85.8 nM (IC₅₀); ALK4: 2133 nM (IC₅₀); ALK5: 9276 nM (IC₅₀)

References

[1] mohedas a h, xing x, armstrong k a, et al. development of an alk2-biased bmp type i receptor kinase inhibitor. acs chemical biology, 2013, 8(6): 1291-1302.

LDN212854 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from LDN212854 manufacturers

Career Henan Chemical Co

Product: LDN212854 1432597-26-6
Price: US $1.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 100KG
Release date: 2019-12-20

1432597-26-6, LDN212854Related Search:

LDN-212320 LDN-193189 HCl LDN-214117 5-[6-(4-Methoxyphenyl)pyrazolo[1,5-a] ALK5 inhibitor II SB525334 LDN-193189 K 02288 AT9283

LDN212854

Quinoline, 5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-

BMP Inhibitor III

5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyriMidin-3-yl]quinoline

CS-1202

BMP INHIBITOR III;LDN212854;LDN 212854

5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline LDN 212854

LDN 212854 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline

LDN-212854, >=98%

LDN-212854 (This product is only available in Japan.)

5-[6-[4-(Piperazin-1-yl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline

LDN212854 USP/EP/BP

LDN-212854 ，S7147

1432597-26-6

1432587-26-6

Inhibitors