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Serine/threonin kinase Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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. SP600125 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. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):987
S7083 Ceritinib Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
Cancer Discov, 2024, OF1-OF20.
Nat Commun, 2024, 15(1):51
Commun Biol, 2024, 7(1):412
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 antitomor activity.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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.
Cancers (Basel), 2024, 16(8)1520
FASEB J, 2024, 38(7):e23604
bioRxiv, 2024, 2024.06.09.598125
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..
Cancers (Basel), 2022, 14(19)4695
Mol Cell, 2020, 80(6):1104-1122.e9
Cell, 2017, 171(7):1545-1558
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.
Sci Rep, 2019, 9(1):382
Nature, 2015, 519(7542):247-50
Nature, 2015, 12;519(7542):247-50.
S8810 SPHINX31 SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).
Leukemia, 2023, 37(8):1649-1659
Antiviral Res, 2023, 10.1016/j.antiviral.2023.105756
S8929 GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
Exp Mol Med, 2024, 56(2):408-421.
Respir Res, 2024, 25(1):201
Nat Commun, 2021, 12(1):5507
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. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
Clin Transl Med, 2022, 12(5):e743
S0015 WNK-IN-11 WNK-IN-11 is a potent, selective, and orally acitve allosteric inhibitor of With-No-Lysine (WNK) kinase with IC50 of 4 nM for WNK1 enzyme.
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
E1670New MKI-1 MKI-1(MASTL Kinase Inhibitor-1) is an small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in kinase assay. It also exerts antitumor and radiosensitizer 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.
S8945 BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.
E0380 Hepln-13 Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, 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.
E2987New 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. HPK1-IN-2 exhibits antitumor activity.
E1975New HC-7366 HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumor activity.
S8257New CFI-402257 CFI-402257(Luvixasertib) is an inhibitor of threonine tyrosine kinase (TTK) with 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 mobilizing immune cells from the tumor microenvironment.
S6088 6-(Dimethylamino)purine 6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.
S0431 ML281 ML281 is a potent and selective inhibitor of Serine/threonine kinase 33 (STK33) with IC50 of 0.014 μM. ML281 is selectively toxic to KRAS-dependent cancer cell lines.
iScience, 2024, 27(3):109300
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.
E1065 SBP-3264 SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).
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. SP600125 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. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2024, 42(4):535-551.e8
Nat Commun, 2024, 15(1):2581
Nat Commun, 2024, 15(1):987
S7083 Ceritinib Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
Cancer Discov, 2024, OF1-OF20.
Nat Commun, 2024, 15(1):51
Commun Biol, 2024, 7(1):412
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 antitomor activity.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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.
Cancers (Basel), 2024, 16(8)1520
FASEB J, 2024, 38(7):e23604
bioRxiv, 2024, 2024.06.09.598125
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..
Cancers (Basel), 2022, 14(19)4695
Mol Cell, 2020, 80(6):1104-1122.e9
Cell, 2017, 171(7):1545-1558
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.
Sci Rep, 2019, 9(1):382
Nature, 2015, 519(7542):247-50
Nature, 2015, 12;519(7542):247-50.
S8810 SPHINX31 SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).
Leukemia, 2023, 37(8):1649-1659
Antiviral Res, 2023, 10.1016/j.antiviral.2023.105756
S8929 GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
Exp Mol Med, 2024, 56(2):408-421.
Respir Res, 2024, 25(1):201
Nat Commun, 2021, 12(1):5507
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. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
Clin Transl Med, 2022, 12(5):e743
S0015 WNK-IN-11 WNK-IN-11 is a potent, selective, and orally acitve allosteric inhibitor of With-No-Lysine (WNK) kinase with IC50 of 4 nM for WNK1 enzyme.
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
E1670New MKI-1 MKI-1(MASTL Kinase Inhibitor-1) is an small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in kinase assay. It also exerts antitumor and radiosensitizer 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.
S8945 BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.
E0380 Hepln-13 Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, 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.
E2987New 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. HPK1-IN-2 exhibits antitumor activity.
S8257New CFI-402257 CFI-402257(Luvixasertib) is an inhibitor of threonine tyrosine kinase (TTK) with 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 mobilizing immune cells from the tumor microenvironment.
S6088 6-(Dimethylamino)purine 6-Dimethylaminopurine (N,N-Dimethyladenine) is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes.
S0431 ML281 ML281 is a potent and selective inhibitor of Serine/threonine kinase 33 (STK33) with IC50 of 0.014 μM. ML281 is selectively toxic to KRAS-dependent cancer cell lines.
iScience, 2024, 27(3):109300
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.
E1975New HC-7366 HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumor activity.
E1670New MKI-1 MKI-1(MASTL Kinase Inhibitor-1) is an small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in kinase assay. It also exerts antitumor and radiosensitizer activities through PP2A-mediated c-Myc inhibition in breast cancer models.
E2987New 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.
E1975New HC-7366 HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumor activity.
S8257New CFI-402257 CFI-402257(Luvixasertib) is an inhibitor of threonine tyrosine kinase (TTK) with 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 mobilizing immune cells from the tumor microenvironment.

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Tags: STK activation | STK kinase family | STK family kinases | STK activity | STK cancer | Serine/threonine kinase | STK phosphorylation | STK inhibition | STK inhibitors cancer | STK inhibitor review