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Details

Stereochemistry ACHIRAL
Molecular Formula C14H16ClN3O4S2
Molecular Weight 389.878
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of N-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide

SMILES

CC(=O)NC1=NC(C)=C(S1)C2=CC=C(Cl)C(=C2)S(=O)(=O)NCCO

InChI

InChIKey=JFVNFXCESCXMBC-UHFFFAOYSA-N
InChI=1S/C14H16ClN3O4S2/c1-8-13(23-14(17-8)18-9(2)20)10-3-4-11(15)12(7-10)24(21,22)16-5-6-19/h3-4,7,16,19H,5-6H2,1-2H3,(H,17,18,20)

HIDE SMILES / InChI

Description

PIK-93 is the two most potent and multitargeted synthetic PI3-K inhibitors that have been reported. PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 uM, and 0.12 uM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 uM. PIK-93 was identified as a potent anti-enterovirus compound. PIK-93 targeted PI4Kβ to inhibit interaction of viral 3D polymerase and phosphatidylinositol 4-phosphate on the reorganized membrane vesicle for viral replication complex formation. PIK-93 may provide a basis for the design of new classes of therapeutics against viral RNA replication.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
39.0 nM [IC50]
16.0 nM [IC50]
64.0 nM [IC50]
120.0 nM [IC50]
19.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
Unknown
Route of Administration: Unknown
In Vitro Use Guide
In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry.