2. PROTAC Apoptosis Epigenetics
  3. PROTACs Apoptosis SF3B1
  4. PROTAC-O4I2

PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.

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PROTAC-O4I2 Chemical Structure

PROTAC-O4I2 Chemical Structure

CAS No. : 2785323-62-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 176 In-stock
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10 mM * 1 mL in DMSO USD 176 In-stock
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5 mg USD 160 In-stock
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Based on 1 publication(s) in Google Scholar

PROTAC-O4I2 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells[1].
PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 exhibits anti-proliferation effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50s 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC-O4I2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: K562 control cells (WT), cells overexpressing SF3B1 (OE), and cells expressing SF3B1K700E (K700E)
Concentration: 1 pM, 0.1 nM, 10 nM, 1 μM, 100 μM
Incubation Time: 72 hours
Result: In K562 WT cells, the parental compound O4I2 exhibited a marginal anti-proliferation effect (IC50 >10 μM). In contrast, PROTAC-O4I2 showed significantly higher toxicity with an IC50 of 228 nM, nearly 3-fold less potent than pladienolide B (IC50, 76 nM). Cells overexpressing SF3B1 WT was slightly resistant to pladienolide B (IC50, 134 nM), but more sensitive to PROTAC-O4I2 (an IC50 value of 63 nM).

Apoptosis Analysis[1]

Cell Line: K562 cell
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced cellular apoptosis s in cells expressing SF3B1WT or SF3B1K700E.
In Vivo

PROTAC-O4I2 (10 μM) significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Drosophila melanogaster[1]
Dosage: 10 μM
Administration: Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days
Result: Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.
Molecular Weight

609.10

Formula

C29H29ClN6O5S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NCCCCCCNC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O)C4=CSC(NC5=CC=C(C=C5)Cl)=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (410.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6418 mL 8.2088 mL 16.4177 mL
5 mM 0.3284 mL 1.6418 mL 3.2835 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.66%

SDS (251 KB)

COA (249 KB) HNMR (145 KB) RP-HPLC (168 KB) LCMS (356 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6418 mL 8.2088 mL 16.4177 mL 41.0442 mL
5 mM 0.3284 mL 1.6418 mL 3.2835 mL 8.2088 mL
10 mM 0.1642 mL 0.8209 mL 1.6418 mL 4.1044 mL
15 mM 0.1095 mL 0.5473 mL 1.0945 mL 2.7363 mL
20 mM 0.0821 mL 0.4104 mL 0.8209 mL 2.0522 mL
25 mM 0.0657 mL 0.3284 mL 0.6567 mL 1.6418 mL
30 mM 0.0547 mL 0.2736 mL 0.5473 mL 1.3681 mL
40 mM 0.0410 mL 0.2052 mL 0.4104 mL 1.0261 mL
50 mM 0.0328 mL 0.1642 mL 0.3284 mL 0.8209 mL
60 mM 0.0274 mL 0.1368 mL 0.2736 mL 0.6841 mL
80 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5131 mL
100 mM 0.0164 mL 0.0821 mL 0.1642 mL 0.4104 mL
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PROTAC-O4I2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC-O4I22785323-62-6PROTACsApoptosisSF3B1Splicing Factor 3b Subunit 1splicing factor 3B1PROTACtargeted protein degradationmolecular degraderprotein-protein interactionSF3B1 inhibitorCRBNThalidomideproteomicsInhibitorinhibitorinhibit

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