Displays 68-fold selectivity over ERα (EC50 values are 2 and 155 for ERβ and ERα respectively). Displays antianxiolytic and antidepressive effects in vivo.
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PPT
PHTPP
DPN
IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively. Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
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Y-27632
Glycyl-H 1152
EC50 values are 240 and 110 nM at human and rat receptors respectively. Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant.
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VU 0155041 sodium salt
MPEP
SIB 1893
Ki = 11 nM, EC50 = 2 nM. Displays no activity at ERα and ERβ at concentration up to 10 μM. Inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro.
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β-Estradiol
ICI 182,780
IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively. Potentiates the effects of radiation, doxorubicin and etoposide in human tumor cell lines in vitro and etoposide in a human tumor xenograft model in vivo.
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Compound 401
DMNB
NU 7441
Scrambled 10Panx,
AM 1172,
Anandamide-d4,
Bendamustine,
G-1,
Gambogic acid,
Goserelin,
GSK 429286,
threo Ifenprodil,
Imiquimod,
K 858,
L-365,260,
Methylphenidate,
NSC 66811,
NU 7441,
Org 12962,
SNAP 94847,
Teijin compound 1,
VU 0238429,
VU 0361737,
WAY 200070
