Serine/threonin kinase

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Serine/threonin kinase Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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.
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.
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 AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Oxid Med Cell Longev, 2022, 2022:2048095
Int J Biol Sci, 2022, 18(5):2047-2059
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.
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.
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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Nature, 2021, 600(7888):319-323
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.
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.
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.
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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 Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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..
Mol Cell, 2020, 80(6):1104-1122.e9
Cell, 2017, 171(7):1545-1558
Nucleic Acids Res, 2017, 45(16):9654-9678
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).
Mol Cancer Ther, 2021, 20(10):1800-1808
BMC Cancer, 2020, 20(1):4
Drug Discov Ther, 2020, 14(5):256-258
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).
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.
S8929 GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
Nat Commun, 2021, 12(1):5507
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.
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.
A5116 Daxx Rabbit Recombinant mAb Daxx Rabbit Recombinant mAb detects endogenous levels of total Daxx.
A5134 CDC5 Rabbit Recombinant mAb CDC5 Rabbit Recombinant mAb detects endogenous level of total CDC5.
A5157 PKN2 Rabbit Recombinant mAb PKN2 Rabbit Recombinant mAb detects endogenous level of PKN2.
A5166 RIP Rabbit Recombinant mAb RIP Rabbit Recombinant mAb detects endogenous level of total RIP.
A5262 Phospho-PAK1/2/3(S144/S141/S139) Rabbit Recombinant mAb Phospho-PAK1/2/3(S144/S141/S139) Rabbit Recombinant mAb detects endogenous level of total Phospho-PAK1/2/3(S144/S141/S139).
A5264 Phospho-RSK1 (S380) Rabbit Recombinant mAb Phospho-RSK1 (S380) Rabbit Recombinant mAb detects endogenous level of total phospho-RSK1 (S380).
A5273 STK3 Rabbit Recombinant mAb STK3 Rabbit Recombinant mAb detects endogenous level of total STK3.
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.
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.
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.
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 AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Oxid Med Cell Longev, 2022, 2022:2048095
Int J Biol Sci, 2022, 18(5):2047-2059
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.
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.
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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Nature, 2021, 600(7888):319-323
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.
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.
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.
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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 Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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..
Mol Cell, 2020, 80(6):1104-1122.e9
Cell, 2017, 171(7):1545-1558
Nucleic Acids Res, 2017, 45(16):9654-9678
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).
Mol Cancer Ther, 2021, 20(10):1800-1808
BMC Cancer, 2020, 20(1):4
Drug Discov Ther, 2020, 14(5):256-258
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).
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.
S8929 GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
Nat Commun, 2021, 12(1):5507
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.
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.
A5116 Daxx Rabbit Recombinant mAb Daxx Rabbit Recombinant mAb detects endogenous levels of total Daxx.
A5134 CDC5 Rabbit Recombinant mAb CDC5 Rabbit Recombinant mAb detects endogenous level of total CDC5.
A5157 PKN2 Rabbit Recombinant mAb PKN2 Rabbit Recombinant mAb detects endogenous level of PKN2.
A5166 RIP Rabbit Recombinant mAb RIP Rabbit Recombinant mAb detects endogenous level of total RIP.
A5262 Phospho-PAK1/2/3(S144/S141/S139) Rabbit Recombinant mAb Phospho-PAK1/2/3(S144/S141/S139) Rabbit Recombinant mAb detects endogenous level of total Phospho-PAK1/2/3(S144/S141/S139).
A5264 Phospho-RSK1 (S380) Rabbit Recombinant mAb Phospho-RSK1 (S380) Rabbit Recombinant mAb detects endogenous level of total phospho-RSK1 (S380).
A5273 STK3 Rabbit Recombinant mAb STK3 Rabbit Recombinant mAb detects endogenous level of total STK3.
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