A p38 MAPK inhibitor
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SCIO 469

Item No. 29484

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-indole-3-acetamide
CAS Number
309913-83-5
Synonyms
  • Talmapimod
Molecular Formula
C27H30ClFN4O3
Formula Weight
513.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
256, 313 nm
SMILES
FC1=CC=C(CN2C[C@@H](C)N(C(C3=CC(C(C(C(N(C)C)=O)=O)=CN4C)=C4C=C3Cl)=O)C[C@@H]2C)C=C1
InChi Code
InChI=1S/C27H30ClFN4O3/c1-16-13-33(17(2)12-32(16)14-18-6-8-19(29)9-7-18)26(35)21-10-20-22(25(34)27(36)30(3)4)15-31(5)24(20)11-23(21)28/h6-11,15-17H,12-14H2,1-5H3/t16-,17+/m0/s1
InChi Key
ZMELOYOKMZBMRB-DLBZAZTESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    SCIO 469 is a p38 MAPK inhibitor (IC50 = 9 nM for p38α).1 It is 10-fold selective for p38α over p38β MAPK and 2,000-fold selective over a panel of 20 additional kinases. SCIO 469 inhibits secretion of IL-6 from multiple myeloma patient-derived bone marrow stromal cells (BMSCs) in a concentration-dependent manner. It increases growth inhibition, DNA fragmentation, and caspase-8 and PARP cleavage induced by the proteasome inhibitor PS-341 (bortezomib; Item No. 10008822) in MM.1S cells when used at concentrations of 100 and 200 nM. SCIO 469 (150 and 450 mg/kg) reduces microvessel density and tumor load and increases survival in a 5T33MM murine myeloma model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hideshima, T., Podar, K., Chauhan, D., et al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene 23(54), 8766-8776 (2004).

    2. Vanderkerken, K., Medicherla, S., Coulton, L., et al. Inhibition of p38α mitogen-activated protein kinase prevents the development of osteolytic bone disease, reduces tumor burden, and increases survival in murine models of multiple myeloma. Cancer Res. 67(10), 4572-4577 (2007).