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New Products
February 2010
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 High affinity and selective GPR30 antagonist
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3678 | G-15
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Ki = 20 nM. Displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive effects of estrogen in vivo.
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Related Products: G-1 ICI 182,780 Tamoxifen
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Selective Pim kinase inhibitor
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3714 | TCS PIM-1 4a
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IC50 values are 24 and 100 nM for Pim-1 and Pim-2 respectively. Displays selectivity over a panel of ~50 other kinases tested. Exhibits cytotoxicity in PC3 prostate carcinoma cells in vitro (IC50 = 17 μM).
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Related Products: PIM-1 Inhibitor 2 TCS PIM-1 1
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Selective mTOR inhibitor
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3725 | KU 0063794
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IC50 ~10 nM for mTORC1 and mTORC2 respectively. Displays no activity at PI 3-K or 76 other kinases tested. Suppresses cell growth and induces G1 cell cycle arrest in vitro.
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Related Products: Compound 401 PI 103 Rapamycin
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Potent, collagenase-selective MMP inhibitor
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2916 | Ro 32-3555
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Ki values are 3.0, 3.4, 4.4, 59, 154 and 527 nM for MMP-1, MMP-13, MMP-8, MMP-9, MMP-2 and MMP-3 respectively. Inhibits cartilage breakdown in vitro and in vivo and displays antiarthritic activity. Orally active.
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Related Products: Batimastat Marimastat UK 370106
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Primes ESCs for differentiation
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3741 | Stauprimide
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Interacts with NME2 and inhibits its nuclear translocation. Increases the efficiency of directed differentiation of mouse and human embryonic stem cells (ESCs) in vitro.
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All new products this month
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CD 2665,
Ceftriaxone,,
Cryptotanshinone,
DADLE,
Disulfiram,
Docosahexaenoic acid,
G-15,
KU 0063794,
L189,
L-DOPA,
MNI-caged-D-aspartate,
Ro 32-3555,
Stauprimide,
SU 3327,
TCS PIM-1 4a,
TNP 470
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