1 | www.apexbt.com LY2228820 Cat. No.: A5566 CAS No.: 862507-23-1 Formula: C24H29FN6·2CH4O3S M.Wt: 612.74 Synonyms: Target: MAPK Signaling Pathway: p38 Storage: Store at -20°C In Vitro ı30.65mg/mL in DMSO, ı9.9 mg/mL in EtOH with ultrasonic, ı45 mg/mL in H2O with ultrasonic Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 1.6320 mL 8.1601 mL 16.3201 mL 5 mM 0.3264 mL 1.6320 mL 3.2640 mL 10 mM 0.1632 mL 0.8160 mL 1.6320 mL Please refer to the solubility information to select the appropriate solvent. Shortsummary P38 MAP kinase inhibitor IC₅₀ & Target 7 nM (p38α) In Vitro Cell Viability Assay Cell Line: HeLa cells Preparation method˖ The solubility of this compound in DMSO is > 30.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. Reacting conditions: 9.8 nM-10 μM, 1 h Applications: LY2228820 is a potent and selective inhibitor of the α- and β-isoforms of p38 Product Name: LY2228820 Revision Date: 01/10/2020 Product Data Sheet Solvent & Solubility Biological Activity 1 | www.apexbt.com L Y2228820 Cat. No.: A556 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 CAS No.: 86 86 6 6 86 6 6 6 86 86 86 86 8 86 86 86 86 8625 25 25 25 25 25 25 25 25 507 07 07 07 07 07 07 07 07 07 7 07 7 - - - - - - 23 2 2 2 2 2 2 2 2 2 2 2 - 1 Formula: C2 C C2 C2 C2 C2 C C C2 C2 C2 C2 C2 C C24H29FN6·2CH4O3S M.Wt: 612.74 Synonyms: T arget: MAPK Signaling Pathway: p38 Storage: Store at - 20°C In Vitro ı ı ı ı ı ı ı ı ı ı ı ı ı ı ı 30.65mg/mL in DMSO, ı 9.9 mg/mL in EtOH with ultrasonic, ı 45 45 45 45 45 45 45 45 45 45 45 45 45 45 45 4 4 m m m m m m m m m m m m m m mg g g g g g g g/ g/ / g/ g/ g/ g g/ / g/ g/ g g g/ g/ / g g mL m m m m m m m m m m in H2O with ultrasonic Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 1.6320 mL 8.1601 mL 16.3201 mL 5 mM 0.3264 mL 1.6320 mL 3.2640 mL 1 0 mM 0.1632 mL 0.81 1 1 1 1 1 1 1 1 160 60 60 60 60 60 60 0 60 60 60 60 6 m m m m m m m m m m mL L L L L L L L L L 1.6320 mL Plea a a a a a a a ase se s se se se se se se e e se e e e e r r r r r r r r r ref ef ef ef ef ef ef ef f e e e e ef e ef e er er er er er er er er er er t t t t t t t t t t to o o o o o o o o o o t t th t t t e solubility information to select the appropriate solvent nt nt t nt t t t nt t. Shortsummary P38 MAP kinase inhibitor IC ₅₀ & Target 7 nM (p38α) In Vitro Cell Viability Assay Cell Line: e: e: e: e: e: e: e e e HeLa cells Pr Pr Pr Pr r Pr Pr Pr Pr Pr P P ep ep ep ep ep ep e ep ep ep ep epar ar a ar ar ar ar ar ar a at at a at at t t t at at t t t at a at t t at ati i i i i io io io i i io io io io io io io o o o o ion n n n n n n n n n n n n method ˖ The solubility of this compound in D D D D D D D D D D D D D D D D DMS MS S S MS S S S MS MS MS MS MS MS MS MS MS MSO O O O O O O O O O O O is is is is is is is is is is is is s > > 30.7 mg/mL. General tips for obtaining a higher concentration: Pl P Pl Pl Pl Pl P Pl Pl Pl Pl P P ea ea ea ea ea ea ea ea ea a ea a ea ea ea ase se se se se se se s se se se se se s warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20°C for several months. Reacting conditions: 9.8 nM - 10 μM, 1 h Applications: LY2228820 is a potent and selective inhibitor of the α - and β - isoforms of p38 Product Name : LY2228820 Revision Date: 0 1 / 1 0 / 0 20 20 et Product Data Shee Solvent & Solu u u u u ub b b b b bi i i i i il l l l l l l l li i i it t t t t t t ty y y y y y y y y y Biologica a a al l l l l l A A A A A A Activity
Transcript
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LY2228820Cat. No.: A5566
CAS No.: 862507-23-1
Formula: C24H29FN6·2CH4O3S
M.Wt: 612.74
Synonyms:
Target: MAPK Signaling
Pathway: p38
Storage: Store at -20°C
In Vitro
30.65mg/mL in DMSO, 9.9 mg/mL in EtOH with ultrasonic, 45 mg/mL in H2O with ultrasonic
Preparing
Stock Solutions
Mass
1mg 5mg 10mgSolvent
Concentration
1 mM 1.6320 mL 8.1601 mL 16.3201 mL
5 mM 0.3264 mL 1.6320 mL 3.2640 mL
10 mM 0.1632 mL 0.8160 mL 1.6320 mL
Please refer to the solubility information to select the appropriate solvent.
Shortsummary P38 MAP kinase inhibitor
IC₅₀ & Target 7 nM (p38α)
In Vitro
Cell Viability Assay
Cell Line: HeLa cells
Preparation method The solubility of this compound in DMSO is > 30.7 mg/mL. General tips for
obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes
and/or shake it in the ultrasonic bath for a while. Stock solution can be stored
below -20°C for several months.
Reacting conditions: 9.8 nM-10 μM, 1 h
Applications: LY2228820 is a potent and selective inhibitor of the α- and β-isoforms of p38
Product Name: LY2228820Revision Date: 01/10/2020
Product Data Sheet
Solvent & Solubility
Biological Activity
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LY2228820Cat. No.: A55666666666666666666666
CAS No.: 868666866668686868688686868686252525252252525252550707070700707070707077077------2322222222222 -1
30.65mg/mL in DMSO, 9.9 mg/mL in EtOH with ultrasonic, 45454545454545454545454545454544 mmmmmmmmmmmmmmmgggggggg/g//g/g/g/gg//g/g/ggg/g//gg mLmmmmmmmmmm in H2O with ultrasonic
Preparing
Stock Solutions
Mass
1mg 5mg 10mgSolvent
Concentration
1 mM 1.6320 mL 8.1601 mL 16.3201 mL
5 mM 0.3264 mL 1.6320 mL 3.2640 mL
10 mM 0.1632 mL 0.81111111111606060606060600606060606 mmmmmmmmmmmLLLLLLLLLL 1.6320 mL
Pleaaaaaaaaasesesseseseseseseeeseeeeese rrrrrrrrrrefefefefefefefeffeeeeefeefe erererererererererer ttttttttttto oooooooooo ttthttt e solubility information to select the appropriate solventntnttnttttntt.
Shortsummary P38 MAP kinase inhibitor
IC₅₀ & Target 7 nM (p38α)
In Vitro
Cell Viability Assay
Cell Line:e:e:e:e:e:e:eee HeLa cells
PrPrPrPrrPrPrPrPrPrPP epepepepepepeepepepepepararaarararararara atataatattttatattttataatttatatiiiiiioioioiiioioioioioioioooooionnn n nnn nnnnnn method The solubility of this compound in DDDDDDDDDDDDDDDDDMSMSSSMSSSSMSMSMSMSMSMSMSMSMSMSO O O O OO O OOOOO isisisisisisisisisisisiss >> 30.7 mg/mL. General tips for
obtaining a higher concentration: PlPPlPlPlPlPPlPlPlPlPP eaeaeaeaeaeaeaeaeaaeaaeaeaeaasesesesesesesesseseseseses warm the tube at 37 °C for 10 minutes
and/or shake it in the ultrasonic bath for a while. Stock solution can be stored
below -20°C for several months.
Reacting conditions: 9.8 nM-10 μM, 1 h
Applications: LY2228820 is a potent and selective inhibitor of the α- and β-isoforms of p38
MAPK with IC50 values of 5.3 and 3.2 nmol/L, respectively. In
anisomycin-stimulated HeLa cells, LY2228820 efficiently inhibited
phosphorylation of p38α MAPK substrate, MK2 (Thr334). LY2228820 also
decreased TNF-α secretion induced by LPS/IFN-γ in mouse peritoneal
macrophages.
In Vivo
Animal experiment
Animal models: Athymic nude female mice
Dosage form: Oral administration, 20 and 40 mg/kg three times daily
Applications: LY2228820 reduced hemoglobin content in athymic nude mice. LY2228820
treatment resulted in a significant reduction of VEGF-A-stimulated
vascularization in an ear angiogenesis model, indicating LY2228820 treatment
impaired neoangiogenesis.
Other notes: Please test the solubility of all compounds indoor, and the actual solubility may
slightly differ with the theoretical value. This is caused by an experimental
system error and it is normal.
1.Jaco I, Annibaldi A,et al. "MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death." MolCell. 2017 Jun
1;66(5):698-710.e5.PMID:28506461
See more customer validations on www.apexbt.com.
[1]. Campbell R M, Anderson B D, Brooks N A, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38
MAPK with antitumor activity[J]. Molecular cancer therapeutics, 2014, 13(2): 364-374.
[2]. Tate C M, Blosser W, Wyss L, et al. LY2228820 dimesylate, a selective inhibitor of p38 mitogen-activated protein kinase, reduces
angiogenic endothelial cord formation in vitro and in vivo[J]. Journal of Biological Chemistry, 2013, 288(9): 6743-6753.
FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.Specific storage and handling information for each product is indicated on the product datasheet. Most APExBIO products are stable
under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage
temperature. Shortterm storage of many products are stable in the short-term at temperatures that differ from that required for
long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt
of the product, follow the storage recommendations on the product data sheet.
Product Citations
References
Caution
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MAPK with IC50 values of 5.3 and 3.2 nmol/L, respectively. In
anisomycin-stimulated HeLa cells, LY2228820 efficiently inhibited
phosphorylation of p38α MAPK substrate, MK2 (Thr334). LY2228820 also
decreased TNF-α secretion induced by LPS/IFN-γ in mouse peritoneal
treatment resulted in a significant reduction of VEGF-A-stimulated
vascularization in an ear angiogenesis model, indicating LY2228820 treatment
impaired neoangiogenesis.
Other notes: Please test the solubility of all compounds indoor, and the actual solubility may
slightly differ with the theoretical value. This is caused by an experimental
system error and it is normal.
1.Jaco I, Annibaldi A,et al. "MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death." MolCell. 2017 Jun
1;66(5):698-710.e5.PMID:28506461
See more customer validations on www.apexbt.com.
[1]. Campbell R M, Anderson B D,D,D,D,D,DD,D,D BBBBBBBBBBBBrororororororororororrookokokokokokokkokokks ss s ss s s sss N A, et al. Characterization of LY2228820 dimesylate, a pooteteetetetetetetetenttttttttttttttttt aaaaaaaaaandndndnddndndndndndndn ssssssssssselelelelelelelelelellee ective inhibitor of p38
MAPK with antitumor activiiiiitytytytytytytytytyyy[J[J[J[J[J[J[J[J[[J[JJJJJJ[J].].].].].]].].].]] MMMMMMMMMMMMMMMMMMolololololololololollecececececececececeece ular cancer therapeutics, 2014, 13(2): 364-374.
[2]. Tate C M, Blosser WWWWWWWWWWW,,,,,,, WyWyWyWyWyWyWyWyWyWyWysssssssssssssssssssssssss LLLLLLLLLLLL, et al. LY2228820 dimesylate, a selective inhibitor of p3888888888888888 mmmmmmmmmmmmmmmmititititititititititttiti ogogogogogogogogogogoooooooo enenenenenenenenenenennn-------aaacaaaaaaaaa tivated protein kinase, reduces
angiogenic endototototottototttto hehehehehehehehehehehehehehehehelililililililililililiaaaaalalallalalaalaaa ccccccccccccccorororororoorororororooo ddddddddddd formation in vitro and in vivo[J]. Journal of Biological Chemiststststtststststststtststttryryryryryryryryryryryryryryryyr ,,,,,,,,,,, 202022202220222222 13, 288(9): 6743-6753.
FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTTIC USE.Specific storage and handling infoofooofoooooofoformrrmrmrmrmrmrmrmrrmatatatatatatatatatatioioioioioioioioiooooon nnnnnnnnn for each product is indicatted on the product datasheet. MoMoMoMoMoMoMoMoMoMoMM sststssssssstststststttsttsttstss AAAAAAAAAAAAAAAAAAAAPEPEPEPEPEPEPEPEPEPEPEEEPEPPPPPPPPPP xBxBxBxBxxBxBBxxBxBxxxEEEEEEEEEEEE IO ble products are stab
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