Inhibitor of G2 DNA damage checkpoint (IC50=8µM) and check point kinases 1 (Chk1) (IC50=3µM) and 2 (Chk2) (IC50=3.5µM). Unlike other checkpoint inhibitors DBH does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related protein. Also inhibits MAP kinase kinase 1 (MEK-1) (IC50=881nM) but is not as potent as 10Z-hymenialdisine (IC50=6nM).
Product Details
| Alternative Name: | DBH, 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one |
| |
| Formula: | C11H11N5O2 |
| |
| MW: | 245.2 |
| |
| Source: | Isolated from sponge Axinella carteri. |
| |
| CAS: | 75593-17-8 |
| |
| Purity: | ≥95% (HPLC) |
| |
| Identity: | Determined by 1H-NMR and MS. |
| |
| Appearance: | Yellow solid. |
| |
| Solubility: | Soluble in 100% ethanol or DMSO. |
| |
| Shipping: | Ambient Temperature |
| |
| Long Term Storage: | -20°C |
| |
| Handling: | Protect from light. Keep under inert gas. |
| |
| Regulatory Status: | RUO - Research Use Only |
| |
Please mouse over
Product Literature References
G2 checkpoint abrogators as anticancer drugs: T. Kawabe; Mol. Cancer Ther.
3, 513 (2004),
Abstract;
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem.
45, 529 (2002),
Abstract;
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem.
276, 17914 (2001),
Abstract;
Full Text
