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Enzastaurin (LY317615) - ≥98%, high purity , Protein kinase C beta inhibitor, CAS No.170364-57-5, Protein kinase C beta inhibitor

  • Moligand™
  • ≥98%
Item Number
E125760
Grouped product items
SKUSizeAvailabilityPrice Qty
E125760-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$75.90
E125760-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$151.90
E125760-250mg
250mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$684.90

Potent PKCβ inhibitor

Basic Description

SynonymsEnzastaurin|170364-57-5|LY317615|Enzastaurin (LY317615)|3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione|LY-317615|3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrro
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent PKCβinhibitor (IC50values are 6, 39, 83 and 110 nM for PKCβ, PKCα, PKCγand PKCε, respectively). Suppresses proliferation and induces apoptosis in HCT116 colon carcinoma and U87MG glioblastoma cellsin vitro. Reduces tumor growth and exhibits antiang
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionProtein kinase C beta inhibitor
Note卖完停产,不再备货
Product Description

Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε.
A potent inhibitor of PKCβ, PKCα, PKCγ and PKCε.

Product Properties

ALogP3.7

Names and Identifiers

IUPAC Name 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
INCHI InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)
InChi Key AXRCEOKUDYDWLF-UHFFFAOYSA-N
Canonical SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7
Isomeric SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7
WGK Germany 3
PubChem CID 176167
Molecular Weight 515.6

Certificates

Certificate of Analysis(COA)

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2 results found

Lot NumberCertificate TypeDateItem
B1526033Certificate of AnalysisJun 12, 2024 E125760
L2325048Certificate of AnalysisJan 03, 2024 E125760

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 10.31, Max Conc. mM: 20
SensitivityMoisture Sensitive

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H413:May cause long lasting harmful effects to aquatic life

H302:Harmful if swallowed

Precautionary Statements

P273:Avoid release to the environment.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

WGK Germany 3

Related Documents

References

1. Teicher BA, Alvarez E, Menon K, Esterman MA, Considine E, Shih C, Faul MM.  (2002)  Antiangiogenic effects of a protein kinase Cbeta-selective small molecule..  Cancer Chemother Pharmacol,  49  (1): (69-77).  [PMID:11855754]
2. Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M.  (2003)  Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta..  Bioorg Med Chem Lett,  13  (11): (1857-9).  [PMID:12749884]
3. Graff JR, McNulty AM, Hanna KR, Konicek BW, Lynch RL, Bailey SN, Banks C, Capen A, Goode R, Lewis JE et al..  (2005)  The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts..  Cancer Res,  65  (16): (7462-9).  [PMID:16103100]

Solution Calculators