Home > Products > Featured products

GSK-25

  Cat. No.:  DC8520   Featured
Chemical Structure
874119-56-9
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 874119-56-9
Chemical Name: 4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide
SMILES: CC1=C(C(N=C(N1)C2=CC(=NC=C2)Cl)C3=C(C=C(C=C3)Cl)F)C(=O)NC4=C(C=C5C(=C4)C=NN5)F
Formula: C24H16Cl2F2N6O
M.Wt: 513.32
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].
Target: ROCK1:7 nM (IC50) RSK1:398 nM (IC50) p70S6K:1000 nM (IC50)
In Vitro: GSK-25 (Rat aorta IC50=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure[1]. GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey)[1].
References: [1]. Sehon CA, et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC74557 PREX-in1 PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
DC74555 GYS32661 GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
DC74539 L557-0155 L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.
DC74528 K284 K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.
DC74225 YB-537 YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).
DC74218 UT-59 UT-59 is a specific inhibitor of cholesterol-sensing membrane protein Scap, binds to Scap's cholesterol-binding site, blocks SREBP activation and inhibits lipid synthesis.
DC74205 Tryptolinamide Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive
DC74198 TMX-4102 TMX-4102 (TMX4102) is a highly potent, selective PIP4K2C binder with KD of 0.45 nM, shows no affinity for PIP4K2B and PIP4K2A (KD>10 uM).
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia