About 24 results found for searched term "CK2-IN-9" (0.126 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M45305 | CK2-IN-9 | Casein Kinase |
| CK2-IN-9 is a potent selective inhibitor of CK2 kinase with an IC50 of 3 nM, and also reduces the reporter activity of Wnt with an IC50 of 75 nM. In addition, CK2-IN-9 is characterized by low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) in rats. | ||
| M49883 | Nickel,dibromo[1,2-ethanediylbis[diphenylphosphine-kP]]-, (SP-4-2)- (9CI) | Others |
| Nickel,dibromo[1,2-ethanediylbis[diphenylphosphine-kP]]-, (SP-4-2)- (9CI) | ||
| M2255 | Genistein | EGFR/HER2 |
| NPI 031L | ||
| Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. | ||
| M3412 | Propafenone hydrochloride | Sodium Channel |
| Propafenone HCl is a sodium-channel blocker that also has a high affinity for β-receptors (IC50 = 32 nM). It blocks transient outward potassium current (Ito) and sustained delayed rectifier K+ current (Isus) with IC50 values of 4.9 μM and 8.6 μM, respectively.In addition, Propafenone inhibits the proliferation of esophageal cancer by inducing mitochondrial dysfunction and apoptosis. | ||
| M3486 | NPS-2143 | Calcium-sensing Receptor |
| SB262470 | ||
| NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. | ||
| M6970 | ML171 | NADPH Oxidase |
| 2-Acetylphenothiazine; 2-APT | ||
| ML171 is a potent and selective inhibitor of NADPH-oxidase with IC50s of 0.25 μM, 5 μM, 3μM, 5 μM and 5.5 μM for NOX1, NOX2, NOX3, NOX4 and xanthine oxidase, respectively. ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay. | ||
| M7690 | ML-9 | Autophagy |
| ML-9 is a potent, selective Akt kinase inhibitor that inhibits myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. It acts on MLCK, PKA and PKC with Ki values of 4, 32 and 54 μM, respectively. In addition, ML-9 induces autophagy by stimulating the formation of autophagosomes and inhibiting their degradation. | ||
| M7901 | LY-294,002 hydrochloride | PI3K |
| LY294002 hydrochloride | ||
| LY-294,002 hydrochloride is a potent broad-spectrum PI3K inhibitor with IC50s of 0.5, 0.57, and 0.97 μM for P110α, P110δ, and P110β, respectively; in addition, LY294002 hydrochloride also inhibits CK2, with an IC50 of 98 nM, and can be used in studies related to pancreatic cancer. LY294002 hydrochloride can also inhibit CK2 with an IC50 of 98 nM. | ||
| M8121 | PD-85639 | Others |
| PD-85639 (PD85,639) is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1. | ||
| M29862 | KRAS inhibitor-9 | Ras |
| KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells. | ||
| M29950 | BT2 | Bcl-2 |
| BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM. | ||
| M30426 | Bepridil | Calcium Channel |
| (±)-Bepridil; Org 5730 | ||
| Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells. | ||
| M30518 | ARP-100 | MMP |
| ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM). | ||
| M30744 | TC-E 5001 | PARP |
| TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively. | ||
| M30803 | SC99 | STAT |
| SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities. | ||
| M30952 | Lck inhibitor 2 | Src-bcr-Abl |
| Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1] Target: Src family kinase Lck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM). | ||
| M41415 | CK1-IN-2 | Casein Kinase |
| CK1-IN-2 is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively. | ||
| M41592 | THK01 | ROCK |
| THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. | ||
| M45287 | CK2/ERK8-IN-1 | Casein Kinase |
| CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) (Ki 0.25 µM) and ERK8 (MAPK15, ERK7), both with IC50s of 0.50 µM. In addition, CK2/ERK8-IN-1 binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. 15.25 µM and 11.9 µM, respectively, and also has pro-apoptotic activity. | ||
| M45289 | CK2 inhibitor 2 | Casein Kinase |
| CK2 inhibitor 2 is a potent, selective and orally active CK2 inhibitor with an IC50 value of 0.66 nM.CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2 and possesses good anti-proliferative and anti-tumor activity. | ||
| M45307 | Multi-kinase-IN-6 | Casein Kinase |
| Multi-kinase-IN-6 is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1 and CDK2. In addition, Multi-kinase-IN-6 also showed antiproliferative activity against MCF7, HCT116 and EKVX, with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively, and showed good apoptotic activity in MCF7 and HCT116 cells with cell-cycle arrest in G1/S and G1 phases. phase, with good apoptosis effect. | ||
| M45310 | SR-1277 | Casein Kinase |
| SR-1277 is a potent, selective and ATP-competitive CK1δ/ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.In addition, SR-1277 inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. 1340 nM, 311 nM and 109 nM, respectively, and can be used in cancer research. | ||
| M49543 | ROCK-IN-6 | ROCK |
| ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. | ||
| M52796 | Verticilide | Calcium Channel |
| Verticilide is a ryanodine-binding inhibitor and inhibits ryanodine binding to ryanodine receptors in the cockroach at an IC50 value of 4.2 μM (whereas inhibition against mouse ryanodine receptors was weak (IC50=53.9 μM)). | ||
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