A marine sponge alkaloid that inhibits Chk1 and Chk2 (IC50 = 3 and 3.5 µM

Debromohymenialdisine – 100 µg

Brand:
Cayman
CAS:
75593-17-8
Storage:
-20
UN-No:
Non-Hazardous - /

Damaged DNA in humans is detected by sensor proteins that transmit a signal through checkpoint kinases (Chks) Chk1 and Chk2.{24026} Debromohymenialdisine (DBH) is a marine sponge alkaloid that inhibits Chk1 and Chk2 (IC50 = 3 and 3.5 µM, respectively), blocking G2 arrest.{24024,24029} Because it does not significantly affect the activity of ataxia-telangiectasia mutated (ATM) or ATM-Tad2-related protein, DBH is a useful tool for studying the roles of Chk1 and Chk2 in DNA repair and cell cycle regulation.{24024} DBH also inhibits MAP kinase kinase 1 (IC50 = 881 nM), glycogen synthase kinase 3β (IC50 = 1.39 μM), cyclin-dependent kinase 5/p25 (IC50 = 9.12 μM), protein tyrosine kinase 6 (IC50 = 0.6 μM), and other kinases largely unrelated to DNA damage/repair and cell cycling.{24027,24028,24025,24023}  

 

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Description

A marine sponge alkaloid that inhibits Chk1 and Chk2 (IC50 = 3 and 3.5 µM, respectively), blocking G2 arrest; also inhibits MEK-1 (IC50 = 881 nM), GSK3β (IC50 = 1.39 μM), Cdk5/p25 (IC50 = 9.12 μM), Brk (IC50 = 0.6 μM), and other kinases largely unrelated to DNA damage/repair and cell cycling

Formal name: (4Z)-4-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-4,5,6,7-tetrahydro-pyrrolo[2,3-c]azepin-8(1H)-one

Synonyms:  DBH|SKF 108753

Molecular weight: 245.2

CAS: 75593-17-8

Purity: ≥95%

Formulation: A yellow solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling

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