LDN-193189 化学構造
分子量: 406.48

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製品説明

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製品の説明

生物活性

製品説明 LDN-193189は、ALK2ALK3の選択的な阻害剤で、IC50がそれぞれ5 nMと30 nMです。
ターゲット ALK2 ALK3
IC50 5 nM [1] 30 nM [1]
In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
C2C12 NUX6cXJtU2mwYYPlJGF{e2G7 MlLMbY5pcWKrdIOgeIhmKGurbnHz[UBi[3Srdnn0fUBw\iCDTFu0JIFv\CCDY4TSTWlCKHerdHigTWM2OMLidnHseYV{KG:oIEGwNUBidmRiMkGwJI5uNCC{ZYPw[YN1cX[nbIm= M1fmUFI2OzZ6M{Ky
EOC216 MmjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWwMlEuOTBizszN Mmi2Nk0yOCCm NGHYNnRFVVOR NUGzbFVvcW6mdXPlJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NH3ZVlIzPTJ{N{i5Ny=>
OVAC429 NE[4RmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[4RWdROi93IN88US=> NU\PSWxSPDhiaB?= NFjJdo5FVVOR MXnk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| M3jMVlI2OjJ5OEmz
SKOV3 NEfOT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG4Nk82KM7:TR?= MY[0PEBp NU\RdpFnTE2VTx?= NXW0Tmpk\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> NHnPfnMzPTJ{N{i5Ny=>
OVCA429 NHnOVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWyM|Uh|ryP NFHFSnc1QCCq M3jEZWROW09? MlLE[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= NYq3RnY2OjV{Mke4PVM>
EOC219 MoTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojvNk82KM7:TR?= MUG0PEBp MUPEUXNQ NVzMN3VE\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MWqyOVIzPzh7Mx?=
A549 Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz1[JgxNjVvMU[g{txO NGHXfWlFVVOR MmTnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVqyOFc4QDBzMR?=
BEAS-2B  MmXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2SzbVAvPS1zNjFOwG0> MlrXSG1UVw>? NFzIUIJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3fmXFI1Pzd6MEGx
hBMSCs MnTrSpVv[3Srb36gRZN{[Xl? MkP1NE4zyqEQvF2= MXW3JIQ> MYrhZo9tcXOqZYOgeIhmKHOrbHnibY5qdi2ycn;tc5Rm\CCDTGCgZYN1cX[rdIpCpJBienSueR?= NWW1V3p5OjRyN{[xPFc>
PANC-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XFb|UuPTByIH7N MVm0PEBp M{G1bYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGGzPZYzOzl4OUeyPS=>
MIA PaCa-2 NHXjeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rHTVUuPTByIH7N Mk[2OFghcA>? NUDxdZVqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGH5WnAzOzl4OUeyPS=>
Bx-PC3 NGPPRVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfkPZk2NTVyMDDuUS=> M3PYN|Q5KGh? MmfIbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWnkRllEOjN7Nkm3Nlk>
PC3  MVvGeY5kfGmxbjDBd5NigQ>? MnXNOVAxKG6P NGS2UHEzKGh? M3Xtc5JmeHKnc4Pld{Bi[3SrdnH0bY9vKG:oIGPtZYQyNzVxODDhcoQhWC2VbXHkN{Bt\X[nbIO= MVyyNlQ2Ojh6Mx?=
LNCaP MUXGeY5kfGmxbjDBd5NigQ>? M1;tZ|DjiJN3MECgcm0> NX[2b|Y3OiCq NEPmUnNz\X[ncoPld{Bz[XCjbYnjbY4ucW6mdXPl[EBk\WyuIHTlZZRp NWjPflk1OjJ2NUK4PFM>
EOC M4qwfWZ2dmO2aX;uJGF{e2G7 NF3qcGIyOC1zMECwJI5O M2[4blczKGh? NX3l[HlFemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0[YQhSk2SIGKtV41i\DFxNT:4xsA> MUmyNlI1QTRzNR?=
HaCaT  NEXjcHZHfW6ldHnvckBCe3OjeR?= NFnaZ5gxNjByMT2xNEDPxE1? M1jsNFIhcA>? MmDjbY5pcWKrdIOgRm1ROi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkNU82Nzhid3n0bEBidiCLQ{WwxsBw\iC-MD6wNFXDqM7:TR?= M3rzbVIyPzRyOU[2
HaCaT  MV\GeY5kfGmxbjDBd5NigQ>? M2La[VAvODBzLUGwJO69VQ>? MVSyJIg> NIP5cZdqdmirYnn0d{B1cGViYXLpcIl1gSCxZjDBUGszKHSxIIDoc5NxcG:{eXzheIUhT1OWLWPtZYQyyqC5aYToJIFvKEmFNUFCpI9nKDR3wrDuUS=> M{PGNlIyPzRyOU[2
HaCaT  M3KxT2Z2dmO2aX;uJGF{e2G7 NXq2dIVPOC5yMEGtNVAh|ryP MWOyJIg> M2\Y[4lvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|MhfG9icHjvd5Bpd3K7bHH0[UBUdWGmMdMge4l1cCCjbjDJR|UxyqCxZjCxNFAhdk1? MVeyNVc1ODl4Nh?=
HaCaT  Moi5SpVv[3Srb36gRZN{[Xl? NXvpWFJtOC5yMEGtNVAh|ryP NIPoXGkzKGh? NVfLVJR{cW6qaXLpeJMhSUyNNDDhcoQhSUyNNTD3bZRpKEmFNUFCpJZidHWnczDv[kAxNjQEoN88UUBidmRiMD61xsDPxE1icnXzdIVkfGm4ZXz5 NEDRNmszOTd2MEm2Oi=>

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [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.

動物実験: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download LDN-193189 SDF
分子量 406.48
化学式

C25H22N6

CAS No. 1062368-24-4
保管 2年-20℃
6月-80℃in solvent
別名 DM3189
溶解度 (25°C) * In vitro DMSO <1 mg/mL (<1 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo Saline (suspension) 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

文献中の引用 (12)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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