STO609 structure
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Common Name | STO609 | ||
|---|---|---|---|---|
| CAS Number | 52029-86-4 | Molecular Weight | 314.29 | |
| Density | N/A | Boiling Point | 797.3ºC at 760 mmHg | |
| Molecular Formula | C19H10N2O3 | Melting Point | >300ºC | |
| MSDS | N/A | Flash Point | 436ºC | |
Use of STO609STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. |
| Name | STO-609 acetate,7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylicacidacetate |
|---|---|
| Synonym | More Synonyms |
| Description | STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. |
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| Related Catalog | |
| Target |
Ki: 80 ng/mL (CaM-KKα), 15 ng/mL (CaM-KKβ)[1] |
| In Vitro | STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/mL, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC50 value of the compound against CaM-KII is 10 μg/mL. STO-609 inhibits constitutively active CaM-KKα as well as the wild-type enzyme. In transfected HeLa cells, STO-609 suppresses the Ca2+-induced activation of CaM-KIV in a dose-dependent manner. STO-609 significantly reduces the endogenous activity of CaM-KK in SH-SY5Y neuroblastoma cells at a concentration of 1μg/mL (80% inhibitory rate)[1]. |
| Kinase Assay | CaM-KI (2.5 μg/mL), CaM-KII (0.75 μg/mL), CaM-KIV (9 μg/mL), and mLCK (0.6 μg/mL) are incubated with 40 μM syntide-2 or 50 μM mLC peptide (for mLCK) at 30 °C for 5 min in a solution (25 μL) containing 50 mM HEPES (pH 7.5), 10 mM Mg(Ac)2, 1 mM DTT, 50 μM [γ-32P]ATP (4500 cpm/pmol) with various concentrations of STO-609 (0–10 μg/mL)in Me2SO at a final concentration of 4%) in the presence of 1 mM CaCl2, 2 μM CaM. Protein kinase activity is measured by the phosphocellulose filter method. Specific activities of CaM-KI, CaM-KII, CaM-KIV, and mLCK in the absence of STO-609 are calculated[1]. STO-609 is bound in the ATP-binding pocket of the CaMKKβ KD. The inhibition mechanism of STO-609 is ATP-competitive[2]. |
| References |
| Boiling Point | 797.3ºC at 760 mmHg |
|---|---|
| Melting Point | >300ºC |
| Molecular Formula | C19H10N2O3 |
| Molecular Weight | 314.29 |
| Flash Point | 436ºC |
| PSA | 108.97000 |
| LogP | 3.38100 |
| Appearance of Characters | yellow solid |
| InChIKey | MYKOWOGZBMOVBJ-UHFFFAOYSA-N |
| SMILES | O=C(O)c1ccc2c3c1cccc3c(=O)n1c3ccccc3nc21 |
| Storage condition | -20℃ |
| Safety Phrases | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| HS Code | 2933990090 |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Name: Cytotoxicity activity against human HepG2 cells assessed by CellTiter-Glo luminescent...
Source: ChEMBL
Target: HepG2
External Id: CHEMBL5303715
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Name: Primary qHTS for inhibitors of NSP2Pro chikungunya virus (CHIKV)
Source: NCGC
External Id: APP-Toga-CHIKV-nsp2-p
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Name: Millipore: Percentage of residual kinase activity of PRKAA2 at 10uM relative to contr...
Source: ChEMBL
Target: 5'-AMP-activated protein kinase catalytic subunit alpha-1
External Id: CHEMBL2219380
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Name: Millipore: Percentage of residual kinase activity of NUAK1 at 1uM relative to control...
Source: ChEMBL
Target: NUAK family SNF1-like kinase 1
External Id: CHEMBL2219381
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|
Name: Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to contr...
Source: ChEMBL
Target: 5'-AMP-activated protein kinase catalytic subunit alpha-1
External Id: CHEMBL2219378
|
|
Name: Millipore: Percentage of residual kinase activity of PRKAA2 at 1uM relative to contro...
Source: ChEMBL
Target: 5'-AMP-activated protein kinase catalytic subunit alpha-1
External Id: CHEMBL2219379
|
|
Name: Millipore: Percentage of residual kinase activity of MAP3K5 at 10uM relative to contr...
Source: ChEMBL
Target: Mitogen-activated protein kinase kinase kinase 5
External Id: CHEMBL2218943
|
|
Name: Millipore: Percentage of residual kinase activity of ABL1 at 1uM relative to control....
Source: ChEMBL
Target: Tyrosine-protein kinase ABL1
External Id: CHEMBL2218944
|
|
Name: Millipore: Percentage of residual kinase activity of NUAK1 at 10uM relative to contro...
Source: ChEMBL
Target: NUAK family SNF1-like kinase 1
External Id: CHEMBL2219382
|
|
Name: Millipore: Percentage of residual kinase activity of MAP3K5 at 1uM relative to contro...
Source: ChEMBL
Target: Mitogen-activated protein kinase kinase kinase 5
External Id: CHEMBL2219383
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| sto-609 |
| sto-609 acetic acid |
| sto-609 acetate |