Search results for '1.'
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PF 04885614
PF 04885614 is a potent NaV1.8 inhibitor (IC50 = 53 nM for human NaV1.8 channel), which exhibits selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNaV1.2 and hNaV1.5 (IC50 values are 4.2, 7.0, 11, 16 and 27 μM respectively). Learn MoreStarting at: $125.00
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PI 828
PI 828 is a PI 3-Kinase inhibitor with IC50 values of 0.098, 0.183, 0.227 and 1.967 μM for p110β, p110α, p110δ and p110γ respectively. Learn MoreStarting at: $69.00
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CI 898 trihydrochloride
CI 898 trihydrochloride is a potent lipophilic inhibitor of dihydrofolate reductase (DHFR) that inhibits protozoal, bacterial and human DHFR with IC50 values of 1.4, 6.1 and 3.2 nM respectively. Learn MoreStarting at: $139.00
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NSC 109555 ditosylate
NSC 109555 ditosylate is a selective, reversible, ATP-competitive Chk2 inhibitor that displays no effect on a range of other kinases including Chk1. Learn MoreStarting at: $119.00
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PD 334581
PD 334581, an analog of PD 184352, is an inhibitor of MEK1. Learn MoreStarting at: $198.00
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PIT 1
PIT 1, a selective PIP3 antagonist, blocks the binding of PIP3 to the pleckstrin homology (PH) domain of Akt (IC50 = 31.03;M) and also inhibits cancer cell survival and induces apoptosis by inhibition of PIP3-dependent PI 3-kinase/Akt signaling. Learn MoreStarting at: $119.00
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LY 311727
AM 630 is a CB2 antagonist/inverse agonist (Ki = 31.2 nM) that displays 165-fold selectivity over CB1 receptors. Learn MoreStarting at: $140.00
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SB 590885
SB 590885 is a potent B-Raf inhibitor (Kd = 0.3 nM), which is elective for B-Raf against 46 other kinases (Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively), and decreases anchorage-independent growth of melanoma cell lines. It also inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. Learn MoreStarting at: $159.00
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BRD 7389
BRD 7389 is a p90 ribosomal S6 kinase (RSK) inhibitor (IC50 values are 1.2, 1.5 and 2.4 μM for RSK3, RSK1 and RSK2 respectively), which upregulates insulin expression in terminally differentiated pancreatic α-cells. Learn MoreStarting at: $139.00
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SSR 69071
SSR 69071 is a high affinity, potent inhibitor of human leukocyte elastase (HLE) (IC50 = 3.9 nM), which displays species-selectivity (Ki values are 0.017, 1.70, 3.01, 58 and > 100 nM for human, mouse, rat, rabbit and porcine elastase respectively) and inhibits HLE-induced lung hemorrhage in mice (ID50 = 2.8 mg/kg) and reduces infarct size in an in vivo acute model of coronary ischemia-reperfusion injury. Orally active. Learn MoreStarting at: $139.00
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BPIPP
BPIPP is a non-competitive guanylyl cyclase (GC) and adenylyl cyclase (AC) inhibitor, which downregulates cAMP and cGMP synthesis, and suppresses cGMP accumulation in a variety of cell lines (IC50 = 3.4 - 11.2 μM). It also inhibits GC-stimulated Cl- transport in vitro and suppresses toxin-induced intestinal fluid accumulation in vivo. Learn MoreStarting at: $145.00
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IBMX
IBMX is a phosphodiesterase inhibitor (IC50 values are 13, 18, 19, 32 and 50 μM for PDE4, PDE3, PDE1, PDE5 and PDE2 respectively) which suppresses α-adrenoceptor-mediated 5-HT release from neuroendocrine epithelial cells (IC50 = 1.3 μM). Learn MoreStarting at: $59.00
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DCA
DCA is an inhibitor of mitochondrial pyruvate dehydrogenase kinase (PDK), which shifts pyruvate metabolism from glycolysis and lactate production to glucose oxidation in the mitochondria, and induces mitochondrial-dependent apoptosis and reverses the inhibition/downregulation of KV1.5 channels in cancer but not normal cells. Learn MoreStarting at: $55.00
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ABT 702 dihydrochloride
ABT 702 dihydrochloride is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase). Learn MoreStarting at: $180.00
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m-3M3FBS
m-3M3FBS is a activator of phospholipase C (PLC), which stimulates superoxide generation, Ca2+ release and inositol phosphate formation in a variety of cell types, and inhibits growth of the leukemic cell lines U937 and THP-1. Learn MoreStarting at: $98.00
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TBB
TBB is a cell-permeable, selective inhibitor of casein kinase-2 (CK2) (IC50 = 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively). Learn MoreStarting at: $65.00
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SQ 22536
SQ 22536 is an inhibitor of adenylyl cyclase (IC50 = 1.4 μM) which inhibits PGE1-stimulated increases in cAMP levels in intact human platelets. Learn MoreStarting at: $98.00
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CP 80633
CP 80633 is a selective inhibitor of phosphodiesterase type 4 (IC50 values are 1.9, > 100, > 100, > 100 and > 100 μM for human lung PDE4, lung PDE1, lung PDE2, heart PDE3 and platelet PDE-V respectively) that displays no significant PDE4 isozyme selectivity. Learn MoreStarting at: $135.00
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Mirin
Mirin is a mre11-Rad50-Nbs1 (MRN)-ATM pathway inhibitor that blocks the 3' and 5' exonuclease activity associated with Mre11. It also blocks homology-directed repair in vitro. Learn MoreStarting at: $95.00
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CZC 54252 hydrochloride
CZC 54252 hydrochloride is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) (IC50 values are 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively). Learn MoreStarting at: $145.00