2. Epigenetics
  3. Histone Acetyltransferase
  4. KI-TOX-A3

KI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC50 of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8+ T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL.

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KI-TOX-A3

KI-TOX-A3 Chemical Structure

CAS No. : 1351116-34-1

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Based on 1 publication(s) in Google Scholar

KI-TOX-A3 Related Antibodies

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Description

KI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC50 of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8+ T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL[1].

In Vitro

KI-TOX-A3 (0.156-10 μM) potently inhibits the TOX-KAT7 protein-protein interaction in cell-free ELISA assays, with an IC50 of 0.51 μM[1].
KI-TOX-A3 (100 μM) binds directly to purified full-length TOX protein in cell-free ITC assays, with a Kd value of 1.05 μM[1].
KI-TOX-A3 (0.15-10 μM) binds directly to biotinylated full-length recombinant human TOX protein in cell-free SPR assays, with a Kd of 0.92 μM[1].
KI-TOX-A3 (20-40 μM) selectively competes for binding to TOX protein in Molt-4 cell lysates[1].
KI-TOX-A3 (0-10 μM) dose-dependently restores TOX protein-inhibited KAT7-mediated H3K14 acetylation in cell-free in vitro assays[1].
KI-TOX-A3 (5-10 μM; 24 h) inhibits the protein-protein interaction between TOX and KAT7 in Molt-4 T-ALL cells[1].
KI-TOX-A3 (96 h) exerts selective cytotoxicity against TOX-dependent T-ALL and CTCL cell lines, with IC50 values ranging from 2.0 μM to 6.3 μM after 96 h of treatment, whereas it shows much lower toxicity against TOX-independent cell lines[1].
KI-TOX-A3 (10 μM) induces S-phase cell cycle arrest in Jurkat T-ALL cells[1].
KI-TOX-A3 (5-10 μM; 4-12 h) induces proteasome-dependent degradation of TOX protein in Molt-4 T-ALL cells[1].
KI-TOX-A3 (0.625-10 μM; 2-12 h) dose-dependently reduces TOX mRNA levels in Jurkat T-ALL cells[1].
KI-TOX-A3 (2.5-10 μM; 24 h) reduces the expression of exhaustion markers TIM-3 and LAG-3, promotes the expression of effector cytokines, upregulates PD-1 expression in exhausted primary human CD8+ T cells, restores the cytotoxic activity of exhausted primary human CD8+ T cells against CD19+ Ramos cells, and restores the acetylation level of H3K14 in exhausted primary human CD8+ T cells to a level comparable to that of non-exhausted T cells[1].

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

KI-TOX-A3 Related Antibodies

Western Blot Analysis[1]

Cell Line: Molt-4 T-ALL cells
Concentration: 5 μM, 10 μM
Incubation Time: 0, 2, 4, 6, 8, 12 h (10 μM); 12 h (5 μM, 10 μM)
Result: Reduced TOX protein levels after 4 h of treatment at 10 μM; the proteasome inhibitor MG132 (HY-13259) (1 μM) rescued TOX protein levels in cells treated with 5 μM or 10 μM KI-TOX-A3 for 12 h, indicating proteasome-dependent degradation.

Real Time qPCR[1]

Cell Line: Jurkat T-ALL cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 2, 4, 6, 8, 12 h
Result: Decreased TOX mRNA levels in a dose-dependent manner after 12 h of treatment; significant reductions in mRNA levels were observed after 4 h of 10 μM treatment, with further decreases over time.

Cell Cytotoxicity Assay[1]

Cell Line: Exhausted primary human CD8+ T cells, CD19+ Ramos cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Restored cytotoxic activity of exhausted CD8+ T cells against CD19+ Ramos cells, with ~50% improved killing efficiency compared to DMSO-treated exhausted T cells.
Molecular Weight

319.31

Formula

C18H13N3O3
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

OCC1=CC=C(C2=C(CC3=C4C=CC(O)=C3)C4=NC(N)=C2C#N)O1
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 : 4.17 mg/mL (13.06 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 3.1318 mL 15.6588 mL 31.3175 mL
5 mM 0.6264 mL 3.1318 mL 6.2635 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

Purity: 99.15%

SDS (251 KB)

COA (252 KB) HNMR (345 KB) RP-HPLC (206 KB) MS (68 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 3.1318 mL 15.6588 mL 31.3175 mL 78.2938 mL
5 mM 0.6264 mL 3.1318 mL 6.2635 mL 15.6588 mL
10 mM 0.3132 mL 1.5659 mL 3.1318 mL 7.8294 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:

KI-TOX-A31351116-34-1Histone AcetyltransferaseHATsHATTOX protein-protein interaction inhibitorT-ALL cellsCD8+ T cellMolt-4 cellRamos cellsJurkat T-ALL cellsacute lymphoblastic leukemiaInhibitorinhibitorinhibit

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