LY2228820 化学構造
分子量: 612.74



Quality Control & MSDS


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製品説明 LY2228820は、p38 MAPKの新しくて強力な阻害剤で、 IC50 が7 nMになる。
ターゲット p38α
IC50 7 nM [1]
In vitro試験 LY2228820 inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC50 values of 7 nM and 34.3 nM, respectively. Furthermore, LY2228820 inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. [1] In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, LY2228820 (200 nM–800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. LY2228820 (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone doesn't inhibit the growth of MM.1S cells. LY2228820 (200 nM–800 nM) also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138 or PB CD14+ cells. LY2228820 (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
RPMI-8226 NVj6WItiU2mwYYPlJIF{e2G7 MmLSglgxOCCwTR?= NIn4NHdFVVOR NG[wVYhqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= M2jEfFE5Ozl5M{S1
U266 M1j2bmtqdmG|ZTDhd5NigQ>? MWj+PFAxKG6P NUDDWWZqTE2VTx?= M1G1NIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NVznbYtvOTh|OUezOFU>
MM.1S Mm\1T4lv[XOnIHHzd4F6 NUHEb3dxhjhyMDDuUS=> MnPaSG1UVw>? NV;LWo9xcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 M3jofFE5Ozl5M{S1
RPMI-Dox40 MlO3T4lv[XOnIHHzd4F6 MVn+PFAxKG6P MlLCSG1UVw>? MlT0bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 MWWxPFM6PzN2NR?=
RPMI-LR5 NXPNUoFLU2mwYYPlJIF{e2G7 M1qxOZ45ODBibl2= NUXicpdkTE2VTx?= Mmn3bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NGPrfoQyQDN7N{O0OS=>
INA-6 Mom4T4lv[XOnIHHzd4F6 M1WwU545ODBibl2= MlziSG1UVw>? M4rB[olvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NYrmc|c5OTh|OUezOFU>
RPMI-8226 NIrxeFJEgXSxeHnjbZR6KGG|c3H5 MYH+NVAxOCCwTR?= NXu5TYh2TE2VTx?= MXvuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NHXPNm8yQDN7N{O0OS=>
U266 NIr2[ZBEgXSxeHnjbZR6KGG|c3H5 M1HU[p4yODByIH7N MonKSG1UVw>? MXLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NFjHd5UyQDN7N{O0OS=>
MM.1S NGjkZ3dEgXSxeHnjbZR6KGG|c3H5 MnO0glExODBibl2= MmjrSG1UVw>? MXzuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3r0[FE5Ozl5M{S1
RPMI-Dox40 NIfONlNEgXSxeHnjbZR6KGG|c3H5 NWPsdYxnhjFyMECgcm0> MVHEUXNQ MmjFco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M{PWUVE5Ozl5M{S1
RPMI-LR5 Ml7WR5l1d3irY3n0fUBie3OjeR?= MmnwglExODBibl2= M2\LPWROW09? NHLWcHRvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> MWixPFM6PzN2NR?=
INA-6 NGfjbmVEgXSxeHnjbZR6KGG|c3H5 MljDglExODBibl2= NELV[|dFVVOR M{foV45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M2nE[|E5Ozl5M{S1
CD14+ NWP2WlhRTnWwY4Tpc44h[XO|YYm= MUD+PFAxKG6P M4jvV2ROW09? NIjqVW9qdmirYnn0d{Bwe3Snb3PsZZN1d2enbnXzbZMh\nKxbTDDSFE1KHCxc3n0bZZmKGOnbHzz M2\ZflE5Ozl5M{S1
U-87-MG NYLhVWx5TnWwY4Tpc44h[XO|YYm= NXPBUIlZOSEQvF2= MmSzSG1UVw>? NGnBbmdz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MWSyN|M{PTVyNh?=
MDA-MB-231 NHe0UY9HfW6ldHnvckBie3OjeR?= MljoNUDPxE1? MYXEUXNQ NEWzeotz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> NVfaNJY6OjN|M{W1NFY>
A-2780 MWPGeY5kfGmxbjDhd5NigQ>? NGjVfFkyKM7:TR?= MYTEUXNQ M130WpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NHXrcFkzOzN|NUWwOi=>
SK-OV-3 MmP2SpVv[3Srb36gZZN{[Xl? MmixNUDPxE1? NX:3WHN6TE2VTx?= NILFW2Vz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> NF6zT2YzOzN|NUWwOi=>
LXFA-629 MoHuSpVv[3Srb36gZZN{[Xl? NHT6cGcyKM7:TR?= MWjEUXNQ MYny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NUnSPW1pOjN|M{W1NFY>
NCI-H1650 M2i3[WZ2dmO2aX;uJIF{e2G7 MUOxJO69VQ>? MXTEUXNQ NWW5coVEemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NHSxOWczOzN|NUWwOi=>
PC-3 M{\jTWZ2dmO2aX;uJIF{e2G7 MlzxNUDPxE1? M4O0ZWROW09? NYTo[W5kemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MmG2NlM{OzV3ME[=
RAW264.7 M3vMcmZ2dmO2aX;uJIF{e2G7 NH[xNXR,OjBizszN NVnVbZJFTE2VTx?= MXfpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= MYiyOFM2PjhzNB?=
mouse peritoneal macrophages NIex[IFHfW6ldHnvckBie3OjeR?= NEDjemp,OjBizszN M33KWWROW09? NWfteZlyVFCVL1nGUk3Pu+LCk4P0bY12dGG2ZXSgWG5HNc7zIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDZwMzDuUS=> M1njeVI1OzV4OEG0
A549 MYHGeY5kfGmxbjDhd5NigQ>? M1roNp4zOCEQvF2= NVfMc3pyTE2VTx?= Mo\ZbY5pcWKrdIOgUHBUNWmwZIXj[YQhS1iFTEigdJJw\HWldHnvckB4cXSqIFnDOVAhd2ZiMUS0Mlkhdk1? M331dlI1OzV4OEG0
MDA-231 MYHGeY5kfGmxbjDhd5NigQ>? NXztdYRShjFyIN88US=> MoXHd5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u M2LUXlI3PDB5OESz
MCF-7 MojJSpVv[3Srb36gZZN{[Xl? NFWzR3J,OTBizszN NULwfGRre3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NH7zOmIzPjRyN{i0Ny=>
MDA-435 M3:yZmZ2dmO2aX;uJIF{e2G7 MoTkglExKM7:TR?= MWfzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MUKyOlQxPzh2Mx?=
PC3 M4niRmZ2dmO2aX;uJIF{e2G7 MYr+NVAh|ryP MWjEUXNQ M2noZpN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NF\XNIEzPjlzM{[wPC=>

... Click to View More Cell Line Experimental Data

In vivo試験 In LPS-induced mice, LY2228820 effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED50) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), LY2228820 displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED50)of 1.5 mg/kg. [1]
臨床試験 LY2228820 is currently under a Phase I clinical trial for the treatment of advanced cancer.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Inhibition of p38α Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-33P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.

細胞アッセイ: [2, 3]

細胞株 MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40
濃度 200 nM–800 nM
反応時間 48 hours
実験の流れ MTT assays and APO 2.7 staining are performed to assess cellular proliferation and induction of apoptosis, respectively. Viability is expressed as percent viable cells. Apoptosis in cells is evaluated by APO 2.7 staining. For detection of mitochondrial membrane protein 7A6 expressed in apoptotic cells, cells are incubated with APO 2.7 reagent for 20 min. Expression of APO 2.7 is determined using an EPICS XL flow cytometer.

動物実験: [1]

動物モデル Lipopolysaccharide (LPS)-induced Balb/c mice
製剤 Dissolved in 1% CMC/0.25% Tween 80 in water
投薬量 0–20 mg/kg
投与方法 Oral bid dosing for 14 days

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
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)



Download LY2228820 SDF
分子量 612.74


CAS No. 862507-23-1
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 4 mg/mL warming (6.52 mM)
100 mg/mL warming (163.2 mM)
エタノール 3 mg/mL (4.89 mM)
In vivo Saline 30 mg/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 5-(2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine dimethanesulfonate

文献中の引用 (9)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID