LY2228820
- CAS NO.:862507-23-1
- Empirical Formula: C26H37FN6O6S2
- Molecular Weight: 612.7369832
- MDL number: MFCD22572532
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-04 13:44:46
What is LY2228820?
The Uses of LY2228820
LY2228820 is a novel and potent p38MAPK inhibitor with potent antiinflammatory activity. LY2228820 significantly inhibited phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, in both multiple myeloma (MM) cell lines and LT-BMSCs. LY2228820 is a potential candidate to improve MM patient outcome both by enhancing the effect of Bortezomib (B675700) and by reducing osteoskeletal events.
What are the applications of Application
LY2228820 is SB 202190 is a p38 MAP Kinase inhibitor with IC50 of 70nM
Biological Activity
ly2228820 is a potent, selective, atp-competitive small-molecule inhibitor inhibiting α- and β-isoforms of p38 mapk with ic(50) values of 5.3nm and 3.2 nm, respectively1.in multiple myeloma (mm) cell lines, ly2228820 enhanced the cytotoxicity of bortezomiba via reducing bortezomib-induced phosphorylation of heat shock protein 27 (hsp27). ly2228820 significantly reduced il-6 secretion from bm mononuclear cells (bmmncs) and long term cultured-bm stromal cells (lt-bmscs). besides, ly2228820 can also inhibit secretion of macrophage inflammatory protein-1a (mip-1a) in bmmncs, cd138+ patient mm cells and normal cd14+ osteoclast cells 2.studies in mice implanted with b16-f10 melanoma showed that orally administered ly2228820 can effectively suppress the tumor-phospho-mk2 expression. treatment of ly2228820 caused a significant tumor growth delay in a549 nsclc xenograft models1.
References
1. campbell rm1, anderson bd, brooks na, brooks hb, chan em, de dios a, gilmour r, graff jr, jambrina e, mader m, mccann d, na s, parsons sh, pratt se, shih c, stancato lf, starling jj, tate c, velasco ja, wang y, ye xs.characterization of ly2228820 dimesylate, a potent and selective inhibitor of p38 mapk with antitumor activity. mol cancer ther. 2014 feb;13(2):364-74.2. ishitsuka k1, hideshima t, neri p, vallet s, shiraishi n, okawa y, shen z, raje n, kiziltepe t, ocio em, chauhan d, tassone p, munshi n, campbell rm, dios ad, shih c, starling jj, tamura k, anderson kc. p38 mitogen-activated protein kinase inhibitor ly2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. br j haematol. 2008 may;141(5):598-606.
Properties of LY2228820
storage temp. | Store at -20°C |
solubility | ≥30.65 mg/mL in DMSO; ≥45 mg/mL in H2O with ultrasonic; ≥9.9 mg/mL in EtOH with ultrasonic |
form | solid |
color | White to yellow |
Safety information for LY2228820
Computed Descriptors for LY2228820
New Products
(R)-(-)-2-Amino-1-propanol Tetrahydro-4H-pyran-4-one Bromine 99.5% AR (4 x 500ml) Linseed Oil Extrapure Hydrogen Sulphide Solution Oxalic Acid 0.05 mol/L (0.01N) Solution EDTA 0.1 mol/L (0.2N) for 1000 ml Ferroin 0.025M Solution AR 1,2,3,4-Tetrahydrocarbazol-4-one 4-Hydroxy Carbazole Amino Salicylic Acid. U.S.P. 2 – Methoxy – 5- Sulfamoyl Benzoic acid Acetone Isobutryl oxime ester Sodium Amino Salicylate Dihydrate (PAS Sodium) IP/BP/USP/EP Aloe vera extract 200x Withania somnifera (Ashwagandha Extract) Citrus bioflavonoids Extract Spirulina (Arthrospira platensis) Powder Trikatu Extract Thymol Oil Ethyl 3-(Pyridin-2-Ylamino)Propanoate Bilastine -IP/BP/ Cypermethric Acid Chloride 5-NitrosalicylaldehydeRelated products of tetrahydrofuran
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