Serine/threonin kinase Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S8358 | WNK463 | WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4) with IC50 of 5nM, 1nM, 6nM, and 9nM. |
|
|
| S8929 | GCN2iB | GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM. |
|
|
| S7270 | SRPIN340 | SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases. |
|
|
| S4956 | Benzamidine HCl | Benzamidine is an inhibitor of serine proteases with Ki values of 35, 350, and 220 µM for trypsin, plasmin, and thrombin, respectively. |
|
|
| S8810 | SPHINX31 | SPHINX31 is a SRPK1 inhibitor with an IC50 of 5.9 nM with high selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold). |
|
|
| S8945 | BAY-1816032 | BAY-1816032 is a potent and orally available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with an IC50 of 6.1 nM for the recombinant catalytic domain of human BUB1. This compound has antitumour activity. |
|
|
| S0431 | ML281 | ML281 is a potent and selective inhibitor of Serine/threonine kinase 33 (STK33) with an IC50 of 0.014 μM. This compound is selectively toxic to KRAS-dependent cancer cell lines. |
|
|
| S8976 | DCLK1-IN-1 | DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. This compound inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively. |
|
|
| S6710 | SGC-GAK-1 | SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase. |
|
|
| S0015 | WNK-IN-11 | WNK-IN-11 is a potent, selective, and orally active allosteric inhibitor of With-No-Lysine (WNK) kinase with IC50 of 4 nM for WNK1 enzyme. | ||
| E1670 | MKI-1 | MKI-1 (MASTL Kinase Inhibitor-1) is a small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in a kinase assay. It also exerts antitumor and radiosensitiser activities through PP2A-mediated c-Myc inhibition in breast cancer models. | ||
| E2396 | STK16-IN-1 | STK16-IN-1 is a serine/threonine protein kinase 16 (STK16) inhibitor with an IC50 of 295 nM. | ||
| S3522 | 2OH-BNPP1 | 2OH-BNPP1 is an inhibitor of the kinase activity of BUB1 (budding uninhibited by benzimidazoles-1, BUB1 Mitotic Checkpoint Serine/Threonine Kinase) that can be used for the treatment of cancer. | ||
| E0380 | Hepln-13 | Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, which can be used for the research of metastatic prostate cancer. | ||
| S0995 | BioE-1115 | BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively. | ||
| E2987 | GCN2-IN-1 | GCN2-IN-1 (A-92) is a specific and potent active site inhibitor of general control nonderepressible 2 kinase (GCN2) with an IC50 of <0.3 μM. It can be investigated in research related to diseases involving retroviral integration. | ||
| S8864 | ZT-12-037-01 | ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. | ||
| E1120 | TC-DAPK 6 | TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor with IC50 of 69 and 225 nM against DAPK1 and DAPK3, respectively. | ||
| S0848 | GAK inhibitor 49 | GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with an IC50 of 56 nM. | ||
| S6060 | HPK1-IN-2 | HPK1-IN-2 is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1, a serine/threonine Ste20-related protein kinase), Lck and Flt3 with IC50 of <0.05 μM, IC50 of <0.5 μM and IC50 of <0.05 μM, respectively. This compound exhibits antitumour activity. | ||
| S8257 | Luvixasertib (CFI-402257) | Luvixasertib (CFI-402257) is an inhibitor of threonine tyrosine kinase (TTK) with an IC50 of 1.7 nM and Ki of 0.1 nM, respectively. It is a potential therapeutic for treating hepatocellular carcinoma that works directly by inhibiting cell-cycle checkpoints in cancer cells and indirectly by mobilising immune cells from the tumour microenvironment. | ||
| S6088 | 6-(Dimethylamino)purine | 6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits germinal vesicle breakdown and the meiotic maturation of oocytes. | ||
| S1460 | SP600125 | SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. This compound is also a broad-spectrum inhibitor of serine/threonine kinases including Aurora kinase A, FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. It inhibits autophagy and activates apoptosis. |
|
|
| S7083 | Ceritinib | Ceritinib is a potent inhibitor against ALK with an IC50 of 0.2 nM in cell-free assays. This compound also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3. |
|
|
| S4967 | Ceritinib dihydrochloride | Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitumour activity. |
|
|
| E2836 | ALK inhibitor 1 | ALK inhibitor 1 (compound 17) is a potent pyrimidine ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.