Serine/threonin kinase

Inhibitory Selectivity

Isoform-specific Inhibitors

Serine/threonin kinase Products

Catalog No. 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 AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

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.

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..

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.

S4967New

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.

S6060New

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.

S3522New

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.

S0995New

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.

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.

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.

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 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).

S8929

GCN2iB

GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.

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.

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.

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.

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).

Catalog No. 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 AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

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.

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..

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.

S4967New

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.

S6060New

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.

S3522New

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.

S0995New

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.

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.

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.

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 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).

S8929

GCN2iB

GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.

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.

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.

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.

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).

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