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SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a/p38, SAPK2b/p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $36 | In Stock | |
10 mg | $54 | In Stock | |
25 mg | $85 | In Stock | |
50 mg | $123 | In Stock | |
100 mg | $180 | In Stock | |
1 mL x 10 mM (in DMSO) | $58 | In Stock |
Description | SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a/p38, SAPK2b/p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain. |
Targets&IC50 | PKB:5 μM, SAPK2a/p38:50 nM, SAPK2b/p38β2:500 nM |
In vitro | SB 203580 hydrochloride is a selective ATP-competitive p38 MAPK inhibitor against SAPK2a/p38 IC50=50 nM and SAPK2b/p38β2 IC50=500 nM. [1] 0-30 μM SB 203580 hydrochloride pre-incubation, 1 hr and incubation in the presence of 20 ng/mL IL-2 for 24 hr was able to inhibit the IL-2-induced proliferation of primary human T cells, mouse CT6 T cells, or BAF F7 B cells with IC50 values of 3-5 μM. [2] SB 203580 hydrochloride blocks the phosphorylation of PKB (protein kinase B) with an IC50 of approximately 5 μM. [2] |
In vivo | An exogenous tumor model in female thymus-free Nu/Nu mice, 5 mg/kg/day SB 203580 hydrochloride, was injected intraperitoneally daily for 16 consecutive days, and the tumors in the p38WT group were significantly smaller than those in the p38TM tumors of the parallel treatments after treatment. [3] |
Alias | SB203580 hydrochloride, RWJ64809 hydrochloride, RWJ 64809 hydrochloride, Adezmapimod hydrochloride |
Molecular Weight | 413.9 |
Formula | C21H17ClFN3OS |
Cas No. | 869185-85-3 |
Smiles | Cl.O=S(C=1C=CC(=CC1)C2=NC(C=3C=CN=CC3)=C(N2)C=4C=CC(F)=CC4)C |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 2 mg/mL(4.83 mM), Sonication is recommended. DMSO: 80 mg/mL(193.28 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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