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Datasheet of TPCA-1

Description:
TPCA-1 is potent, selective inhibitor of IKK-2 (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold
selectivity over other kinases and enzymes.
in vitro: In a time-resolved fluorescence resonance energy transfer assay, TPCA-1 inhibits human IKK-2 activity with an IC50 of
17.9 nM. In addition, TPCA-1 is demonstrated to be ATP-competitive. Besides, TPCA-1 exhibits IC50 values of 400 nM and
3600 nM against IKK-1 and JNK3, respectively. TPCA-1 inhibits the production of TNF-, IL-6, and IL-8 in a
concentration-dependent manner, exhibiting IC50 values of 170, 290, and 320 nM, respectively. TPCA-1 inhibits glioma cell
proliferation, as well as TNF-induced RelA (p65) nuclear translocation and NFB-dependent IL8 gene expression. Importantly,
TPCA-1 inhibits IFN-induced gene expression, completely suppressing MX1 and GBP1 gene expression, while having only a
minor effect on ISG15 expression.
in vivo: Prophylactic administration of TPCA-1 at 3, 10, or 20 mg/kg, i.p., b.i.d., results in a dose-dependent reduction in the
severity of murine collagen-induced arthritis (CIA). The significantly reduced disease severity and delay of disease onset
resulting from administration of TPCA-1 at 10 mg/kg, i.p., b.i.d. are comparable to the effects of the antirheumatic drug,
etanercept, when administered prophylactically at 4 mg/kg, i.p., every other day. Nuclear localization of p65, as well as levels of
IL-1beta, IL-6, TNF-alpha, and interferon-gamma, is significantly reduced in the paw tissue of TPCA-1- and etanercept-treated
mice. In addition, administration of TPCA-1 in vivo results in significantly decreased collagen-induced T cell proliferation ex
vivo. Therapeutic administration of TPCA-1 at 20 mg/kg, but not at 3 or 10 mg/kg, i.p., b.i.d., significantly reduces the severity
of CIA, as does etanercept administration at 12.5 mg/kg, i.p., every other day.

Chemical Information
Catalog

DC7159

Purity of current batch:

>98%

Molecular Weight (MW)

279.29

Molecular Formula

C12H10FN3O2S

CAS No.

507475-17-4

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.