Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C28H28N4O2 |
| Molecular Weight | 452.5475 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CC1CCN2C3=CC=CC=C3C(=C2C1)C4=C(C(=O)NC4=O)C5=CN(C)C6=C5C=CC=C6
InChI
InChIKey=FXGHOAZJQNLNFD-UHFFFAOYSA-N
InChI=1S/C28H28N4O2/c1-30(2)15-17-12-13-32-22-11-7-5-9-19(22)24(23(32)14-17)26-25(27(33)29-28(26)34)20-16-31(3)21-10-6-4-8-18(20)21/h4-11,16-17H,12-15H2,1-3H3,(H,29,33,34)
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/17212812 | https://www.ncbi.nlm.nih.gov/pubmed/23274455
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/17212812 | https://www.ncbi.nlm.nih.gov/pubmed/23274455
Ro 32-0432 hydrochloride is an orally available cell-permeable selective inhibitor of PKC enzymes. Moreover, Ro 32-0432 inhibits G protein-coupled receptor kinase 5 activity. Ro 32-0432 prevents T cell-driven chronic inflammatory responses in several rat models. Ro 32-0432 inhibits an antigen-driven T-cell-mediated arthritis in vivo. Treatment of rats with Ro 32-0432 in ischemic stroke decreases the ischemic infarction area, neurological symptoms and associated endothelin B receptor upregulation. Ro 32-0432 attenuates the propagation of nicotine dependence and reduce withdrawal signs possibly by G protein-coupled receptor kinase 5 activation-linked mechanisms.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2855 |
9.0 nM [IC50] | ||
Target ID: CHEMBL3020 |
28.0 nM [IC50] | ||
Target ID: CHEMBL3604 |
37.0 nM [IC50] | ||
Target ID: CHEMBL3424 |
108.0 nM [IC50] | ||
Target ID: CHEMBL5678 |
3.0 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effect of Purified Mushroom Tyrosinase on Melanin Content and Melanogenic Protein Expression. | 2016 |
|
| Thrombin-induced IL-8/CXCL8 release is mediated by CK2, MSK1, and NF-κB pathways in human lung epithelial cells. | 2015-11-15 |
|
| Angiotensin II stimulates melanogenesis via the protein kinase C pathway. | 2015-10 |
|
| Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. | 1994-02 |
|
| Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. | 1993-09-01 |
Sample Use Guides
Ro 32-0432 can effectively inhibit IL-2 secretion from T-cells induced by the mitogen PHA in combination with phorbol ester (IC50=30 nM), confirming that Ro 32-0432 is able to gain access into the T-cell cytosol to inhibit PKC-driven responses. Ro 32-0432 nhibited HA27 proliferation with an IC50 of 0.15 uM.
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131848-98-1
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RKX867S6TK
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SUBSTANCE RECORD
