Serine/threonin kinase

Inhibitory Selectivity

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..

S0015New

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.

S7209

GSK650394

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

S8976New

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.

S8929New

GCN2iB

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

S8824New

EMD638683

EMD638683 is a highly selective inhibitor of serum- and glucocorticoid-inducible kinase 1 (SGK1) with IC50 of 3 μM. EMD638683 exhibits antihypertensive potency and anti-tumor activity.

S0431New

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.

S8465

GSK'872 (GSK2399872A)

GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.

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).

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.

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).

S7188

CID755673

CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.

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..

S0015New

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.

S7209

GSK650394

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

S8976New

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.

S8929New

GCN2iB

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

S8824New

EMD638683

EMD638683 is a highly selective inhibitor of serum- and glucocorticoid-inducible kinase 1 (SGK1) with IC50 of 3 μM. EMD638683 exhibits antihypertensive potency and anti-tumor activity.

S0431New

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.

S8465

GSK'872 (GSK2399872A)

GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.

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).

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.

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).

S7188

CID755673

CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.

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