CHIR-99021

SKU: orb1225513

Description

A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively; mimics Wnt signaling in preadipocytes, stabilizes free cytosolic beta-catenin and inhibits adipogenesis by blocking induction of C/EBPα and PPARγ; potentiates insulin activation of glucose transport and utilization in vitro and in vivo; also widely used for stem cell differentiation and naive stem cell generation.(In Vitro):Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM.Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells.Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells.Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes.Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis.(In Vivo):Laduviglusib (30 mg/kg, p.o ) rapidly lowers plasma glucose.Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury.

Key Properties

• CAS Number: 252917-06-9
• MW: 465.3379
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₈Cl₂N₈
• SMILES: CC1=CN=C(N1)C1=CN=C(NCCNC2=NC=C(C=C2)C#N)N=C1C1=C(Cl)C=C(Cl)C=C1
• Target: GSK-3
• Solubility: DMSO: ≥ 5.1 mg/mL

Bioactivity

• In Vitro:
  Laduviglusib (GMP) (20 μM, 21 days) transdifferentiates mouse fibroblasts to neurons (determined by increased number of TAUEGFP-/TUJ1-positive neuronal cells). Laduviglusib (GMP) (3-5 μM, 2 days) induces somatic cells differentiation of pluripotent stem (PS) cells (the detailed method refers to the reference). Laduviglusib (GMP) (12 μM, 5 days) converts human fibroblasts (HFF) into functional cardiomyocytes. Laduviglusib (GMP) (3 μM, 4 days, hESCs) activates the canonical WNT signaling pathway, confirmed by β-catenin translocation into the nucleus. Laduviglusib (GMP) (in MEFs expressing MyoD) enhances the marked increase in the number of proliferative cells led by RepSox (GMP) (HY-13012G) together with Forskolin (HY-15371). Laduviglusib (GMP) (5 μM, 1 day) can be used to generate islets (hCiPSC-islets) from human chemically induced pluripotent stem cells (hCiPSC).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CT99021 | CHIR99021 | CHIR 99021 | CT-99021

Quick Database Links

Gene Symbol

GSK-3