LDN-193189

카탈로그 번호S2618 배치:S261805

인쇄

기술 자료

화학식

C25H22N6
분자량 406.48 CAS 번호 1062368-24-4
용해도 (25°C)* 시험관 내(In vitro) Water 5 mg/mL 50ºC 수조에서 가온 (12.3 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For cell testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
표적
ALK1
(Cell-free assay)		 ALK2
(Cell-free assay)		 ALK3
(Cell-free assay)		 ALK6
(Cell-free assay)
0.8 nM 0.8 nM 5.3 nM 16.7 nM
시험관 내(In vitro)

LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, this compound also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins.

A recent study shows that this chemical blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells.

생체 내(In Vivo)

In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities.

This compound dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development.

In PCa-118b tumor-bearing mice, this chemical treatment attenuates tumor growth and reduces bone formation in the tumors.

In LDL receptor-deficient (LDLR-/-) mice, this agent potently inhibits development of atheroma. Moreover, it also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification.

프로토콜 (참조)

키나아제 분석:

[1]
  • Alkaline phosphatase activity

    C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 days in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 hours and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability and quantity are measured by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements.
세포 분석:

[1]
  • 세포주

    PASMCs 

  • 농도

    5 nM

  • 배양 시간

    12 h

  • 방법

    Cells were treated with various concnetrations of LDN-193189.
동물 연구:

[1]
  • 동물 모델

    Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.

  • 용량

    ≤3 mg/kg

  • 투여

    Administered via i.p.

참조

  • https://pubmed.ncbi.nlm.nih.gov/19029982/
  • https://pubmed.ncbi.nlm.nih.gov/20718746/
  • https://pubmed.ncbi.nlm.nih.gov/21670081/
  • https://pubmed.ncbi.nlm.nih.gov/22223731/
  • https://pubmed.ncbi.nlm.nih.gov/23646137/

고객 제품 검증

<p>LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.</p>

데이터 출처 [ Int J Cancer , 2014 , 136(5):E455-69 ]

<p>The density of muscle fibers and myoseptum are partially rescued in morphants treated with LDN to decrease BMP signaling (D–F) .These were fixed at 24 hpf and labeled with an antibody against Pax7, which strongly labels neural crest derived cells and also labels dermomyotome cells.</p>

데이터 출처 [ Dev Biol , 2014 , 378:107-121 ]

The small molecule BMP inhibitor LDN-193189 can partially block the increased BMP signaling in Jab1flox/flox, Col2a1-Cre mutants in a dose-dependent manner. Primary chondrocytes were cultured in DMEM medium containing 10% FBS and indicated amounts of LDN-193189 for 24 hours before being subjected to immunoblotting.

데이터 출처 [ , , J Cell Sci, 2013, 126: 234-43 ]

(C) Smad1/5/9 phosphorylation and Smad1 protein levels were monitored in BMP-2 stimulated cells for up to 60 min. β-actin served as a loading control; BMP, bone morphogenetic protein.

데이터 출처 [ , , Oncol Rep, 2017, 37(2):713-720 ]

Selleck's LDN-193189 인용됨 275 출판물

HNF1A and A1CF coordinate a beta cell transcription-splicing axis that is disrupted in type 2 diabetes [ Cell Metab, 2025, S1550-4131(25)00334-1] PubMed: 40774250
Acute regulation of murine adipose tissue lipolysis and insulin resistance by the TGFβ superfamily protein GDF3 [ Nat Commun, 2025, 16(1):4432] PubMed: 40360531
FAK signaling suppression by OCT4-ITGA6 mediates the effectively removal of residual pluripotent stem cells and enhances application safety [ Theranostics, 2025, 15(14):7127-7153] PubMed: 40585989
Helicobacter pylori infection induces DNA double-strand breaks through the ACVR1/IRF3/POLD1 signaling axis to drive gastric tumorigenesis [ Gut Microbes, 2025, 17(1):2463581] PubMed: 39924917
DNA hypomethylation at specific CG-sites within TRAK1 is linked to the neurocognitive profile in Klinefelter syndrome [ Mol Psychiatry, 2025, 10.1038/s41380-025-03254-z] PubMed: 41028571
Differential effects of lithium on metabolic dysfunctions in astrocytes derived from bipolar disorder patients [ Mol Psychiatry, 2025, 10.1038/s41380-025-03176-w] PubMed: 40847005
Ex vivo correction of severe coagulation Factor VII deficiency in patient-derived 3D liver organoids [ Haematologica, 2025, 10.3324/haematol.2025.288046] PubMed: 41063698
IPSC-derived organoid-sourced skin cells enable functional 3D skin modeling of recessive dystrophic epidermolysis bullosa [ J Tissue Eng, 2025, 16:20417314251397594] PubMed: 41340774
From inserts to chips: microfluidic culture and 3D astrocyte co-culture drive functional and transcriptomic changes in hiPSC-derived endothelial cells [ Fluids Barriers CNS, 2025, 22(1):58] PubMed: 40524169
Chronic low-dose cadmium exposure induces neurodevelopmental impairment in hESC-derived retinal organoids [ Ecotoxicol Environ Saf, 2025, 305:119189] PubMed: 41072315

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