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PROTAC-O4I2

Catalog No. T74186   CAS 2785323-62-6

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

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PROTAC-O4I2 Chemical Structure
PROTAC-O4I2, CAS 2785323-62-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 54.00
5 mg In stock $ 128.00
10 mg In stock $ 198.00
25 mg In stock $ 455.00
50 mg In stock $ 788.00
100 mg In stock $ 1,280.00
500 mg In stock $ 2,580.00
1 mL * 10 mM (in DMSO) In stock $ 143.00
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Purity: 96.31%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.
In vitro PROTAC-O4I2 introduces thalidomide into the ubiquitin E3 ligase cereblon (CRBN), thereby selectively degrading SF3B1 and inhibiting tumor growth in cells.[1]
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 has anti-proliferative effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50 of 228, 63, and 90 nM, respectively.[1]
PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells.[1]
In vivo Flies were fed on a round filter paper loaded with PROTAC-O4I2 (10 μM) in a 5% sucrose solution, maintained at 18℃, and flipped into a freshly prepared vial every 2 days. PROTAC-O4I2 significantly improves Drosophila survival in a Drosophila intestinal tumor model by interfering with tumor maintenance and proliferation.[1]
Molecular Weight 609.1
Formula C29H29ClN6O5S
CAS No. 2785323-62-6

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (328.35 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Rodrigo A Gama-Brambila, et al. A PROTAC targets splicing factor 3BCell Chem Biol. 2021 Nov 18;28(11):1616-1627.e8.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

PROTAC-O4I2 2785323-62-6 Apoptosis PROTAC PROTACs inhibitor inhibit

 

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