About 18 results found for searched term "SP-96" (0.127 seconds)
Cat.No. | Name | Target |
---|---|---|
M20733 | SP-96 | Aurora Kinase |
SP-146 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-146 can be used for the research of triple negative breast cancer (TNBC). | ||
M2040 | BAY 11-7082 | IκB/IKK |
BAY 11-7821; NF-κB inhibitor 13 | ||
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). | ||
M3773 | PSN 375963 | GPR/FFAR |
PSN-375963 | ||
PSN 375963 is an effective GPR119 agonist with EC50 of 8.4 and 7.9 μM for human and mice, respectively. PSN 375963 showed similar potency to endogenous oleoylethanolamide (OEA). | ||
M6362 | A 196 | Histone Methyltransferase |
A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity. | ||
M13835 | KDM5A-IN-1 | Histone demethylase |
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. | ||
M22527 | Cinchonidine | Alkaloids |
α-Quinidine | ||
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. Cinchonidine (α-Quinidine) is a weak inhibitor of serotonin transporter (SERT) with Ki values of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. | ||
M25388 | 9-Aminocamptothecin | Topoisomerase |
9-amino-CPT; 9-amino-20(S)-camptothecin | ||
9-Aminocamptothecin (9-amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h exposure. | ||
M27936 | BI-9627 | Na+/H+ Exchanger (NHE) |
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury. | ||
M28388 | BI-9627 hydrochloride | Na+/H+ Exchanger (NHE) |
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury. | ||
M28418 | BMS-962212 | Factor Xa |
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity. | ||
M28491 | MRT199665 | Salt-inducible Kinase |
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370. | ||
M29103 | VU6001966 | GluR |
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer. | ||
M30407 | Asperphenamate | Autophagy |
Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively. | ||
M30447 | RU 24969 hemisuccinate | 5-HT Receptor |
RU 24969 hemisuccinate is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion. | ||
M40970 | Hydroethidine | Fluorescent Dye |
Hydroethidine is a peroxide indicator that freely enters cells and dehydrogenates into ethidium bromide and distinguishes between superoxide and H2O2, and can be used to identify proliferating and hypoxic cells in tumors (λex=520 nm, λem=600 nm). This product has been merged into M9696 | ||
M49536 | Rho-Kinase-IN-1 | ROCK |
Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008. | ||
M55637 | TEI-9647 | Vitamin |
TEI-9647 is a Vitamin D3 Lactone analogue, and it is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 blocks both 1α,25(OH)2D3-mediated HL-60 cell differentiation and also activation of the luciferase reporter in COS-7 cells that has been transfected with the cDNA containing the DRE of the rat 25(OH)D3-24-hydroxylase gene and cDNA of the human vitamin D nuclear receptor. | ||
M58399 | F-1 | ALK |
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
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