2. Neuronal Signaling Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. OLIG2 Apoptosis Caspase PARP
  4. CT-179

CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC50 of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G2/M phase arrest and increases G0 population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma.

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CT-179

CT-179 Chemical Structure

CAS No. : 1996636-69-1

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CT-179 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC50 of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G2/M phase arrest and increases G0 population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma[1].

IC50 & Target[1]

Caspase-3

 

PARP

 

In Vitro

CT-179 (10 nM-10 μM; 1 hour) dose-dependently disrupts OLIG2 dimerization in live HEK293 cells, with an IC50 of 1250 nM[1].
CT-179 (1-10 µM; 1 hour) reduces OLIG2-DNA binding in live HEK293 cells, as shown by increased diffusion of DNA-bound OLIG2 and reduced fractional DNA-bound OLIG2 at concentrations of 1 µM and 10 µM[1].
CT-179 (250 nM; 24 hours) blocks OLIG2-driven transcription in Daoy SHH-medulloblastoma cells, as measured by reduced activity of an LHX8 promoter luciferase reporter[1].
CT-179 (1 µM) shows minimal relevant off-target kinase inhibition in vitro; while it inhibits FLT3 with an IC50 of 20 nM in a cell-free assay, the predicted in vivo cell potency is too low to be biologically meaningful[1].
CT-179 (160 nM-2.5 µM) shows minimal off-target effects in normal human primary cells at biologically relevant concentrations (160 nM, 630 nM), with only limited proliferation reduction observed at the supraphysiological concentration of 2.5 µM[1].
CT-179 (1 nM-10 μM; 7 days) reduces viability in OLIG2-expressing SHH-medulloblastoma cell lines (Daoy, UW228, Med-813) in a manner correlating with OLIG2 expression, with IC50 values ranging from 143.6 nM to 965.2 nM, and shows no activity in OLIG2-negative cell lines[1].
CT-179 (1 µM; 17 h-7 days) induces apoptosis, G2/M phase arrest, and mitotic disruption in Daoy SHH-medulloblastoma cells, and potentiates radiotherapy-induced apoptosis[1].
CT-179 (1 µM; 17-96 hours) induces apoptosis and disrupts mitotic mechanisms in Med-813 SHH-medulloblastoma cells, and potentiates radiotherapy-induced apoptosis[1].
CT-179 (1 µM; 48 hours) induces cell death in patient-derived medulloblastoma explant organoids (including SHH-subgroup R902), and when combined with radiotherapy, further reduces proliferation without increasing stem cell populations[1].

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

CT-179 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Daoy SHH-medulloblastoma
Concentration: 1 µM
Incubation Time: 17 h; 24 h; 48 h; 72 h; 96 h; 7 days;
Result: Induced apoptosis, shown by dose-dependent increases in cleaved caspase-3 (cC3) and cleaved PARP over time, and reduced levels of anti-apoptotic proteins MCL-1, BCL-2, and BCL-xL.
Sensitized Daoy cells to RT-induced apoptosis, with significantly higher apoptotic cell percentages in the combination group compared to single-agent treatments on day 1 and day 3.
Induced G2/M phase arrest, decreased cyclin B1, CDK1, and p-CDK1, and maintained elevated p-HH3, resulting in abnormal nuclear morphology (multinucleation, satellite micronuclei) and disrupted mitotic spindle formation.

Apoptosis Analysis[1]

Cell Line: Med-813 SHH-medulloblastoma
Concentration: 1 µM
Incubation Time: 17 h; 24 h; 48 h; 72 h; 96 h
Result: Induced apoptosis, with significantly higher apoptotic cell percentages in the CT-179 and combination groups compared to control on day 3.
Disrupted mitotic mechanisms, with an initial increase in cyclin B1, CDK1, and p-HH3 over 24 hours (accompanied by decreased p-CDK1), followed by decreases in cyclin B1 and CDK1 and a marked increase in p-CDK1 at later time points.
In Vivo

CT-179 (50 mg/kg; i.p.; twice weekly; two weeks) as a single agent prolongs median event-free survival to 60 days, and combination with radiotherapy further extends median event-free survival to 75.5 days while delaying tumor growth in SHH-subgroup medulloblastoma-bearing NRG mice[1].
CT-179 (75 mg/kg; p.o.; every other day) as a single agent prolongs median event-free survival to 76 days, and combination with radiotherapy further extends median event-free survival to 100.5 days in SHH-subgroup medulloblastoma-bearing NRG mice[1].
CT-179 (80 mg/kg; i.p.; every other day) as a single agent reduces tumor proliferation, induces cell cycle arrest and neuronal differentiation, slows tumor growth, and improves event-free survival, while combination with radiotherapy further enhances event-free survival in SHH-subgroup medulloblastoma-bearing G-Smo mice[1].
CT-179 (80 mg/kg; i.p.; every other day) combined with POx-Palbo enhances cell cycle arrest, increases apoptosis, and improves event-free survival more effectively than either single agent in SHH-subgroup medulloblastoma-bearing G-Smo mice[1].

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

Animal Model: NOD-Rag1null IL2rgnull (NRG) (female, 6-7 week-old, orthotopic cerebellar engraftment with Daoy-luci cells)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice weekly; two weeks
Result: Increased median event-free survival (EFS) to 60 days (vs. 55 days for vehicle control).
Increased median EFS to 75.5 days when combined with radiotherapy, which was statistically significant compared to vehicle, CT-179 alone, and radiotherapy alone.
Significantly delayed tumor growth in the brain and spinal cord, with reduced luminescence signal compared to vehicle, CT-179 alone, and radiotherapy alone at day 42.
Animal Model: NOD-Rag1null IL2rgnull (NRG) (female, 6-7 week-old, orthotopic cerebellar engraftment with Med-813-luci cells)[1]
Dosage: 75 mg/kg
Administration: p.o.; every other day
Result: Increased median EFS to 76 days (vs. 71 days for vehicle control).
Increased median EFS to 100.5 days when combined with radiotherapy, which was statistically significant compared to vehicle, CT-179 alone, and radiotherapy alone.
Animal Model: Gfap-Cre/SmoM2 (G-Smo) (genetically engineered SHH-pathway hyperactivation inducing tumor formation by postnatal day 10)[1]
Dosage: 80 mg/kg
Administration: i.p.; every other day
Result: Showed a trend toward decreased phosphorylated OLIG2 (p-OLIG2; p=0.057) and significantly reduced phosphorylated RB (p-RB) in tumors after treatment from P10-P16.
Increased the G2/M fraction at 6 hours after a single dose, and by 24 hours, increased G0 and G2/M fractions with decreased G1 and mitotic (p-RB++) fractions.
Increased NEUN+ neuronal differentiation and OLIG2+/SOX10− tumor stem cell populations, while reducing tumor cross-sectional area at P17.
Significantly improved EFS compared to vehicle controls.
Resulted in statistically significant increased EFS when combined with radiotherapy compared to vehicle, CT-179 alone, and radiotherapy alone.
Animal Model: Gfap-Cre/SmoM2 (G-Smo) (genetically engineered SHH-pathway hyperactivation inducing tumor formation by postnatal day 10)[1]
Dosage: 80 mg/kg plus 25 mg/kg POx-Palbo
Administration: i.p.; every other day
Result: Increased G0 cell fractions, increased G2/M cell fractions (with reduced mitotic p-RB++ cells, indicating G2 arrest), and increased cleaved caspase-3-positive apoptotic cells compared to vehicle, CT-179 alone, and POx-Palbo alone.
Resulted in improved event-free survival compared to either single agent.
Molecular Weight

397.30

Formula

C17H22Cl2N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC(NC(NC2=CC(Cl)=C(C=C2)Cl)=O)=NC(NCCCN(C)C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (31.46 mM; ultrasonic and warming and heat to 60°C; 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 2.5170 mL 12.5849 mL 25.1699 mL
5 mM 0.5034 mL 2.5170 mL 5.0340 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 (protect from light). 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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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: ≥ 1.25 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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 (protect from light). 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 2.5170 mL 12.5849 mL 25.1699 mL 62.9247 mL
5 mM 0.5034 mL 2.5170 mL 5.0340 mL 12.5849 mL
10 mM 0.2517 mL 1.2585 mL 2.5170 mL 6.2925 mL
15 mM 0.1678 mL 0.8390 mL 1.6780 mL 4.1950 mL
20 mM 0.1258 mL 0.6292 mL 1.2585 mL 3.1462 mL
25 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5170 mL
30 mM 0.0839 mL 0.4195 mL 0.8390 mL 2.0975 mL
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  • 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:

CT-1791996636-69-1CT179CT 179OLIG2ApoptosisCaspasePARPOligodendrocyte Transcription Factor 2poly ADP ribose polymeraseHEK293 cellspalbociclibSHH-medulloblastomaNRG miceDaoy SHH-medulloblastoma cellsG-Smo micepatient-derived xenograftcerebellar granule neuronOLIG2+ tumor stem cellsInhibitorinhibitorinhibit

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