PKA

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1113 GSK690693 <1 mg/mL 39 mg/mL '<1 mg/mL
S1573 Fasudil (HA-1077) HCl 65 mg/mL 5 mg/mL '<1 mg/mL
S2670 A-674563 72 mg/mL 72 mg/mL 18 mg/mL
S1582 H 89 2HCl 6 mg/mL 104 mg/mL '<1 mg/mL
S1421 Staurosporine (AM-2282) <1 mg/mL 4 mg/mL ''''''<1 mg/mL
S6214 H-1152 dihydrochloride 78 mg/mL 78 mg/mL ''78 mg/mL
S2964 HA-100 dihydrochloride 70 mg/mL 20 mg/mL ''<1 mg/mL
S2554 Daphnetin <1 mg/mL 35 mg/mL <1 mg/mL
S8388 ML-7 HCl <1 mg/mL 90 mg/mL <1 mg/mL
S0754 Bisindolylmaleimide IV <1 mg/mL 65 mg/mL '''65 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL
S7857 8-Bromo-cAMP 80 mg/mL 5 mg/mL '<1 mg/mL
S7858 Dibutyryl-cAMP (Bucladesine) 98 mg/mL 98 mg/mL ''19 mg/mL

PKA製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1113

GSK690693

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.

S1573

Fasudil (HA-1077) HCl

Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.

S2670

A-674563

A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.

S1582

H 89 2HCl

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.

S1421

Staurosporine (AM-2282)

Staurosporine (AM-2282, Antibiotic AM-2282, STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

S6214

H-1152 dihydrochloride

H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

S2964

HA-100 dihydrochloride

HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.

S2554

Daphnetin

Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.

S8388

ML-7 HCl

ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.

S0754

Bisindolylmaleimide IV

Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8 μM.

S7563

AT13148

AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

S7857

8-Bromo-cAMP

8-bromo-cAMP (8-Br-Camp) is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM; and a PKA activator.

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1113

GSK690693

GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.

S1573

Fasudil (HA-1077) HCl

Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.

S2670

A-674563

A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.

S1582

H 89 2HCl

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.

S1421

Staurosporine (AM-2282)

Staurosporine (AM-2282, Antibiotic AM-2282, STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

S6214

H-1152 dihydrochloride

H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

S2964

HA-100 dihydrochloride

HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.

S2554

Daphnetin

Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.

S8388

ML-7 HCl

ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.

S0754

Bisindolylmaleimide IV

Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8 μM.

S7563

AT13148

AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7857

8-Bromo-cAMP

8-bromo-cAMP (8-Br-Camp) is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM; and a PKA activator.

2021, 19(1):194

2021, 11(1):18532

2021, ioab155

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.

2021, 12(1):4050

2021, e12632

2021, 220:112389