SPHINX31, SRPK1 inhibitor (TBI4376)

Description

Product Details

Formal Name: 5-Pyridin-4-yl-N-[2-[4-(pyridin-2-ylmethyl)piperazin-1-yl]-5-(trifluoromethyl)phenyl]furan-2-carboxamide

Molecular Formula: C₂₇H₂₄F₃N₅O₂

Formula Weight: 507.5

CAS Number: 1818389-84-2

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (15 mg/ml with warming)

Storage: -20°C

Stability: ≥ 2 years.

Applications

SRPK1 inhibitor

Functions

Potent (IC₅₀ = 5.9 nM)  and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), a splice factor kinase involved in VEGF-A isoform formation and other alternative splicing events. It displayed antiangiogenic effects in a mouse model of choroidal neovascularization1 a rat model of diabetic retinopathy. Exhibited antitumor and synergistic (with cisplatin) effects in extranodal lymphoma cells. It was able to change splicing of programmed cell death receptor 1 (PD-1) to produce a more soluble form that prevented T cell exhaustion in a cancer model. It corrected BIN1, MCL-1, and BCL2 splicing errors in cholangiocarcinoma cells resulting in apoptosis of cancer cells.

Application Procedures

First dissolved in DMSO (15 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4376_SPHINX31_datasheet

MSDS:

TBI4376_SPHINX31_MSDS

Research use only.