Serine/threonin kinase

亜型選択性的な製品

serine/threonine kinase STK WNK DCLK GCN GAK SRPK PASK BUB1

Serine/threonin kinase製品

All (24)
Serine/threonin kinase阻害剤 (24)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
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.	Nat Commun, 2024, 15(1):987 Acta Biomater, 2024, S1742-7061(24)00036-9 Cell Death Dis, 2024, 15(1):31
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.	Nat Commun, 2024, 15(1):51 iScience, 2024, 27(2):109015. Clin Cancer Res, 2023, 29(7):1317-1331
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.	Clin Transl Med, 2023, 13(4):e1217 Proc Natl Acad Sci U S A, 2022, 119(30):e2203743119 Cell Rep, 2022, 40(5):111153
S7270	SRPIN340	SRPIN340 is a selective SRPK inhibitor with K_i 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. 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).
E1670^New	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.
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.
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.
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.
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.	Nat Commun, 2024, 15(1):987 Acta Biomater, 2024, S1742-7061(24)00036-9 Cell Death Dis, 2024, 15(1):31
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.	Nat Commun, 2024, 15(1):51 iScience, 2024, 27(2):109015. Clin Cancer Res, 2023, 29(7):1317-1331
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.	Clin Transl Med, 2023, 13(4):e1217 Proc Natl Acad Sci U S A, 2022, 119(30):e2203743119 Cell Rep, 2022, 40(5):111153
S7270	SRPIN340	SRPIN340 is a selective SRPK inhibitor with K_i 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. 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).
E1670^New	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.
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.
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.
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.
E1670^New	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.

Serine/threonin kinase阻害剤の選択性比較