2. Stem Cell/Wnt TGF-beta/Smad Apoptosis
  3. RUNX Apoptosis
  4. RUNX1/ETO-IN-1

RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (KD,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability.

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RUNX1/ETO-IN-1

RUNX1/ETO-IN-1 Chemical Structure

CAS No. : 923865-06-9

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Based on 1 publication(s) in Google Scholar

RUNX1/ETO-IN-1 Related Antibodies

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Description

RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (KD,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability[1].

In Vitro

RUNX1/ETO-IN-1 (Cmpound M23) (96 h) Inhibits cell viability with an IC50 of 62.14 µM in the AML cell line SKNO-1 carrying the t(8;21) translocation that results in RUNX1/ETO[1].

RUNX1/ETO-IN-1 (20-200 µM) reduces the thermal stability of NHR2 (ΔTm = -1.6°C) in a concentration-dependent manner, likely by interfering with the tetramer-dimer equilibrium[1].

RUNX1/ETO-IN-1 (50-100 µM, 24 h) arrests cell cycle and potential induction of apoptosis in SKNO-1 cells, but not in THP-1 cells[1].

RUNX1/ETO-IN-1 (50-100 µM, 24 h) induces apoptosis in SKNO-1 cells by increasing caspase-3 and -7 activity but not in THP-1 and healthy NC-NC control cells[1].

RUNX1/ETO-IN-1 (25-50 µM, 3 days) promotes differentiation in SKNO-1 cells by increasing CD11b expression, but not in K562 and THP-1 cells[1].

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

RUNX1/ETO-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: RUNX1/ETO-negative THP-1, K562, HL-60 cells, RUNX1/ETO-dependent SKNO-1 cells, B-lymphoblastoid cells
Concentration: 1-100 μM
Incubation Time: 72 h
Result: Showed the highest sensitivity to SKNO-1 cells
Affected RUNX1/ETO-negative THP-1, K562, and HL-60 cells slightly
Did not affect B-lymphoblastoid cells

Cell Cycle Analysis[1]

Cell Line: RUNX1/ETO-negative THP-1 and RUNX1/ETO-positive SKNO-1 cells
Concentration: 50, 100 μM
Incubation Time: 24 h
Result: Induced an accumulation in the subG1 and G1 phases, along with a reduction in the S and G2/M phases in the RUNX1/ETO-positive SKNO-1 cells and did not affect the cell cycle phase in the RUNX1/ETO-negative THP-1 cells.
Molecular Weight

399.51

Formula

C21H25N3O3S
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

CC1=CSC2=NC(CNC(C(C)C)C3=CC4=C(OCCCO4)C=C3)=CC(N12)=O
Shipping

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

DMSO : 25 mg/mL (62.58 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 2.5031 mL 12.5153 mL 25.0307 mL
5 mM 0.5006 mL 2.5031 mL 5.0061 mL
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* 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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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. 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 2.5031 mL 12.5153 mL 25.0307 mL 62.5767 mL
5 mM 0.5006 mL 2.5031 mL 5.0061 mL 12.5153 mL
10 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
15 mM 0.1669 mL 0.8344 mL 1.6687 mL 4.1718 mL
20 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
25 mM 0.1001 mL 0.5006 mL 1.0012 mL 2.5031 mL
30 mM 0.0834 mL 0.4172 mL 0.8344 mL 2.0859 mL
40 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5644 mL
50 mM 0.0501 mL 0.2503 mL 0.5006 mL 1.2515 mL
60 mM 0.0417 mL 0.2086 mL 0.4172 mL 1.0429 mL
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RUNX1/ETO-IN-1 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:

RUNX1/ETO-IN-1923865-06-9RUNXApoptosisRunt-related transcription factorsAcute myeloid leukemiaAMLTHP1SKNO-1K562Inhibitorinhibitorinhibit

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