HA-100 hydrochloride

Names

[ Name ]:
HA-100 hydrochloride

[Synonym ]:
5-piperazin-1-ylsulfonylisoquinoline,hydrochloride

Biological Activity

[Description]:

HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor[1][2].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> Myosin

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA

Signaling Pathways >> Stem Cell/Wnt >> PKA

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

PKG:4 μM (IC50)

PKA:8 μM (IC50)

PKC:12 μM (IC50)

MLCK:240 μM (IC50)

ROCK

[In Vitro]

HA-100 hydrochloride inhibits MLC-kinase and PKC competitively with respect to ATP, with Kis of 61 and 6.5 μM, respectively[1].

[References]

[1]. Hagiwara M, et, al. Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives. Mol Pharmacol. 1987 Jul;32(1):7-12.

[2]. Yu J, et, al. Efficient feeder-free episomal reprogramming with small molecules. PLoS One. 2011 Mar 1;6(3):e17557.

Chemical & Physical Properties

[ Boiling Point ]:
497.4ºC at 760 mmHg

[ Melting Point ]:
252-254ºC

[ Molecular Formula ]:
C₁₃H₁₆ClN₃O₂S

[ Molecular Weight ]:
313.80300

[ Flash Point ]:
254.6ºC

[ Exact Mass ]:
313.06500

[ PSA ]:
70.68000

[ LogP ]:
2.97820

Safety Information

[ Hazard Codes ]:
Xi

HA-100 hydrochloride

Names

Biological Activity

Chemical & Physical Properties

Safety Information

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds