General
Preferred name
TASISULAM
Synonyms
LY573636 ()
LY-573636 ()
LY 573636 ()
Tasisulam sodium ()
Tasisulam ()
Tasisulam (LY573636) ()
LY-573636NA ()
LY-573636 SODIUM ()
LY-573636.NA ()
P&D ID
PD010350
CAS
519055-62-0
519055-63-1
Tags
available
molecular glue
PROTAC
drug candidate
Drug Status
investigational
Max Phase
3.0
Drug indication
Acute myeloid leukemia
Melanoma
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization[1].
DESCRIPTION
Tasisulam, also known as LY573636, is an acyl-sulfonamide with potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS). In combination with an angiogenesis inhibitor, this agent may exhibit synergistic antiangiogenic activity.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Tasisulam is a anticancer agent. It inhibits the growth of Calu-6 non-small cell lung carcinoma (NSCLC) and A-375 melanoma cell lines with EC50s = 10 and 25 μM, respectively.
(Enamine Bioactive Compounds)
DESCRIPTION
Tasisulam (LY573636) is an apoptosis inducer and an antitumor agent via the intrinsic pathway.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
16
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
Enamine Bioactive Compounds
Enamine BioReference Compounds
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
MolGlueDB
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
412.83
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
2
Aromatic Ring Count
2
cLogP
3.94
TPSA
63.24
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.83
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Apoptosis
Caspase
Apoptosis inducer
Molecular Glues
Member status
member
MOA
Apoptosis Inducers
apoptosis stimulant
Pathway
Proteases/Proteasome
Source data
