LDN-193189

製品コードS2618 別名:DM3189

LDN-193189化学構造

分子量(MW):406.48

LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

サイズ 価格(税別)  
JPY 18260.00
JPY 28220.00
JPY 94620.00

カスタマーフィードバック(5)

  • 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.

    Int J Cancer 2014 136(5):E455-69. LDN-193189 purchased from Selleck.

    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.

    J Cell Sci, 2013, 126: 234-43. LDN-193189 purchased from Selleck.

  • 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.

    Dev Biol 2014 378:107-121. LDN-193189 purchased from Selleck.

    (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.

    Oncol Rep, 2017, 37(2):713-720. LDN-193189 purchased from Selleck.

  • The influence of SB431542 and LDN193189 on a-SMA in A549 cells. (a) Representative images of immunofluorescence analysis for a-SMA using confocal microscopy are shown (scale bar ¼ 25 lm). (b) Relative densitometry diagram and typical western blot bands of a-SMA expression in the six groups (A–F). Data are expressed as mean ± SD (n ¼ 5 in each group). #p < 0.05 versus CONTROL group, p < 0.05 versus SILICA group

    Toxicol Mech Methods, 2018, 28(4):286-292. LDN-193189 purchased from Selleck.

製品安全説明書

TGF-beta/Smad阻害剤の選択性比較

生物活性

製品説明 LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
ターゲット
ALK2 [1]
(C2C12 cells)
ALK3 [1]
(C2C12 cells)
5 nM 30 nM
体外試験

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, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. [1] A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C2C12 NF\veoVMcW6jc3WgRZN{[Xl? MUTpcohq[mm2czD0bIUhc2mwYYPlJIFkfGm4aYT5JI9nKEGOS{SgZY5lKEGldGLJTWEhf2m2aDDJR|UxyqC4YXz1[ZMhd2ZiMUCxJIFv\CB{MUCgco0tKHKnc4DlZ5RqfmWueR?= NFvGPIgzPTN4OEOyNi=>
EOC216 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIqzUokxNjFvMUCg{txO NUW1ZW53Oi1zMDDk NEe0UpdFVVOR NU[xPJllcW6mdXPlJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkTNNlUzOjd6OUO=
OVAC429 NHr4c3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTFXVEzNzVizszN M4Xx[lQ5KGh? MXTEUXNQ MYHk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NXzTeXJGOjV{Mke4PVM>
SKOV3 NV\0d4hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zVSFIwPSEQvF2= NYnFUHh{PDhiaB?= NFHIU4VFVVOR NUHjSWRx\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MXyyOVIzPzh7Mx?=
OVCA429 NXjuSW83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCyM|Uh|ryP NXK1[3NCPDhiaB?= NHfKUW1FVVOR MnW5[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= NHvKVHQzPTJ{N{i5Ny=>
EOC219 NUPYcJk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH1Nk82KM7:TR?= MmrIOFghcA>? M3nLR2ROW09? NYj2bW9D\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> M{D0O|I2OjJ5OEmz
A549 NHfPRWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3JNE42NTF4IN88US=> MlX1SG1UVw>? NFr1XWhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHiz[ZMzPDd5OECxNS=>
BEAS-2B  NEnkZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17pW|AvPS1zNjFOwG0> NFf6SlRFVVOR MXHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkDkNlQ4PzhyMUG=
hBMSCs NES3b2tHfW6ldHnvckBCe3OjeR?= M4DkblAvOsLizszN M4Dwc|ch\A>? MX7hZo9tcXOqZYOgeIhmKHOrbHnibY5qdi2ycn;tc5Rm\CCDTGCgZYN1cX[rdIpCpJBienSueR?= M1[yVFI1ODd4MUi3
PANC-1 M1m4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK1MVUxOCCwTR?= MWG0PEBp NYWze5J{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGDDXZczOzl4OUeyPS=>
MIA PaCa-2 MmLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn2[4lqPS13MECgcm0> NFGyWZg1QCCq NXTxe453cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHnCbpMzOzl4OUeyPS=>
Bx-PC3 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7OOU02ODBibl2= NITHdWg1QCCq M1TMTolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEXBT|MzOzl4OUeyPS=>
PC3  NWrSS|E3TnWwY4Tpc44hSXO|YYm= NXnhU2xbPTByIH7N NHvYdIwzKGh? MkPadoVxemW|c3XzJIFkfGm4YYTpc44hd2ZiU33h[FEwPS96IHHu[EBRNVOvYXSzJIxmfmWucx?= NVnQbnR[OjJ2NUK4PFM>
LNCaP M{i1R2Z2dmO2aX;uJGF{e2G7 M2X3bVDjiJN3MECgcm0> MkLqNkBp Moq2doV3\XK|ZYOgdoFx[W27Y3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> NYLqN5hYOjJ2NUK4PFM>
EOC NWq1bXlITnWwY4Tpc44hSXO|YYm= NI\JN5UyOC1zMECwJI5O NYX1TWIyPzJiaB?= NGXnVZJz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTl[EBDVVBiUj3TcYFlOS93L{lCpC=> MnTMNlIzPDl2MUW=
HaCaT  NGq0bIdHfW6ldHnvckBCe3OjeR?= M{C3ZlAvODBzLUGwJO69VQ>? MlfzNkBp M4K3T4lvcGmkaYTzJGJOWDJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiU33h[FEwPS96IIfpeIgh[W5iSVO1NOKhd2ZifkCuNFA2yqEQvF2= NX\UepFvOjF5NEC5OlY>
HaCaT  M{DUbmZ2dmO2aX;uJGF{e2G7 MWewMlAxOS1zMDFOwG0> MWqyJIg> NHL4VJFqdmirYnn0d{B1cGViYXLpcIl1gSCxZjDBUGszKHSxIIDoc5NxcG:{eXzheIUhT1OWLWPtZYQyyqC5aYToJIFvKEmFNUFCpI9nKDR3wrDuUS=> M4DhdFIyPzRyOU[2
HaCaT  MUnGeY5kfGmxbjDBd5NigQ>? MkHPNE4xODFvMUCg{txO MX[yJIg> MnfXbY5pcWKrdIOgeIhmKGGkaXzpeJkhd2ZiQVzLN{B1dyCyaH;zdIhwenmuYYTlJHNu[WRzwrD3bZRpKGGwIFnDOVDDqG:oIEGwNEBvVQ>? MViyNVc1ODl4Nh?=
HaCaT  NUPVZ|R7TnWwY4Tpc44hSXO|YYm= MmfXNE4xODFvMUCg{txO NGDWVXAzKGh? NIHtPZhqdmirYnn0d{BCVEt2IHHu[EBCVEt3IIfpeIghUUN3MNMgeoFtfWW|IH;mJFAvO8LizszNJIFv\CByLkZCpO69VSC{ZYPw[YN1cX[nbIm= MW[yNVc1ODl4Nh?=

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体内試験 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. [1] LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2] In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3] In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. [4]

お薦めの試験操作(参考用のみ)

動物試験:[1]
+ 展開
  • 動物モデル: Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
  • 製剤: LDN193189 is dissolved in DMSO and then diluted in water.
  • 投薬量: ≤3 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO Insoluble
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
Saline (suspension)
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 406.48
化学式

C25H22N6

CAS No. 1062368-24-4
保管
in solvent
別名 DM3189

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

TGF-beta/Smadシグナル伝達経路

TGF-beta/Smad Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID