KT5823

KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.

Product information

CAS Number: 126643-37-6

Molecular Weight: 495.53

Formula: C29H25N3O5

Chemical Name: methyl (15S, 16R, 18R)-16-methoxy-4, 15-dimethyl-3-oxo-28-oxa-4, 14, 19-triazaoctacyclo[12.11.2.1, .0, .0, .0, .0, .0, ]octacosa-1, 6, 8, 10, 12, 20, 22, 24, 26-nonaene-16-carboxylate

Smiles: C[C@]12O[C@H](C[C@]1(OC)C(=O)OC)N1C3C(=C4C(=O)N(C)CC4=C4C=3N2C2=CC=CC=C24)C2=CC=CC=C12

InChiKey: QTYMDECKVKSGSM-YMUMJAELSA-N

InChi: InChI=1S/C29H25N3O5/c1-28-29(36-4,27(34)35-3)13-20(37-28)31-18-11-7-5-9-15(18)22-23-17(14-30(2)26(23)33)21-16-10-6-8-12-19(16)32(28)25(21)24(22)31/h5-12,20H,13-14H2,1-4H3/t20-,28+,29+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Gadbois DM, et al. Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells. Proc Natl Acad Sci U S A. 1992 Sep 15;89(18):8626-30.
2. Wyatt TA, et al. KT5823 activates human neutrophils and fails to inhibit cGMP-dependent protein kinase phosphorylation of vimentin. Res Commun Chem Pathol Pharmacol. 1991 Oct;74(1):3-14.
3. Chan SL, et al. Guanylyl cyclase inhibitors NS2028 and ODQ and protein kinase G (PKG) inhibitor KT5823 trigger apoptotic DNA fragmentation in immortalized uterine epithelial cells: anti-apoptotic effects of basal cGMP/PKG. Mol Hum Reprod. 2003 Dec;9(12):775-83.

Products are for research use only. Not for human use.