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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $54 | In Stock | |
5 mg | $128 | In Stock | |
10 mg | $198 | In Stock | |
25 mg | $455 | In Stock | |
50 mg | $788 | In Stock | |
100 mg | $1,280 | In Stock | |
500 mg | $2,580 | In Stock | |
1 mL x 10 mM (in DMSO) | $143 | In Stock |
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 |
Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCCCCCNC(=O)C=4N=C(NC5=CC=C(Cl)C=C5)SC4 |
Storage | keep away from direct sunlight | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 200 mg/mL (328.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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