2. Epigenetics Apoptosis
  3. Histone Acetyltransferase Apoptosis
  4. CHI-KAT8i5

CHI-KAT8i5 is a selective and orally active KAT8 inhibitor with a KD value of 19.72 μM. CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7). CHI-KAT8i5 induces cancer cell apoptosis. CHI-KAT8i5 suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.

For research use only. We do not sell to patients.

CHI-KAT8i5 Chemical Structure

CHI-KAT8i5 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

CHI-KAT8i5 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

CHI-KAT8i5 is a selective and orally active KAT8 inhibitor with a KD value of 19.72 μM. CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7). CHI-KAT8i5 induces cancer cell apoptosis. CHI-KAT8i5 suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway[1].

IC50 & Target

KD value of 19.72 μM for KAT8
In Vitro

CHI-KAT8i5 (0-72 h) inhibits cell proliferation of KYSE 30 and KYSE 150 cells with IC50s of 2-3 μΜ[1].
CHI-KAT8i5 (5-15 μM; 48 h) induces cancer cell apoptosis in a dose-dependent manner[1].
CHI-KAT8i5 (5-15 μM; 12 h) represses the NPM1 and PPAT transcript expression in a dose-dependent manner[1].
CHI-KAT8i5 (2-15 μM; 12 h) shows a dose-dependent decrease in H4K16ace and c-Myc upon[1].

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

CHI-KAT8i5 Related Antibodies

Apoptosis Analysis[1]

Cell Line: KYSE 30 and KYSE 150 cell lines
Concentration: 5 and 15 μM
Incubation Time: 48 h
Result: Could induce cancer cell apoptosis in a dose-dependent manner.

RT-PCR[1]

Cell Line: KYSE 30 and KYSE 150 cell lines
Concentration: 5 and 15 μM
Incubation Time: 12 h
Result: NPM1 and PPAT transcript expression were repressed.

Western Blot Analysis[1]

Cell Line: KYSE 30 and KYSE 150 cell lines
Concentration: 2 μΜ, 4 μΜ, 6 μΜ, 10 μΜ, 15 μΜ
Incubation Time: 12 h
Result: Observed a dose-dependent decrease in H4K16ace and c-Myc.
In Vivo

CHI-KAT8i5 (50-200 mg/kg; oral gavage; once a day; 4-6-week) suppresses ESCC tumor growth in patient-derived ESCC xenografts[1].

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

Animal Model: Six-to eight-week-old severe combined immunodeficient (SCID) female mice were subdermally implanted with LEG379 tumor tissue[1].
Dosage: 50 or 200 mg/kg
Administration: Oral gavage; once a day; 4-6-week
Result: Significantly suppressed tumor growth in the LEG379 (KAT8 high expression levels) case in a dose-dependent manner.
The cell proliferation marker Ki-67 and c-Myc expression were decreased.
The H4K16ace levels were obviously suppressed
Molecular Weight

523.69

Formula

C23H29N3O5S3
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C2N=C(/C=C/C3=CC=C(S(=O)(N(CC)CC)=O)C(O)=C3)SC2=C1)(N(CC)CC)=O
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 : 100 mg/mL (190.95 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 1.9095 mL 9.5476 mL 19.0953 mL
5 mM 0.3819 mL 1.9095 mL 3.8191 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
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 1.9095 mL 9.5476 mL 19.0953 mL 47.7382 mL
5 mM 0.3819 mL 1.9095 mL 3.8191 mL 9.5476 mL
10 mM 0.1910 mL 0.9548 mL 1.9095 mL 4.7738 mL
15 mM 0.1273 mL 0.6365 mL 1.2730 mL 3.1825 mL
20 mM 0.0955 mL 0.4774 mL 0.9548 mL 2.3869 mL
25 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9095 mL
30 mM 0.0637 mL 0.3183 mL 0.6365 mL 1.5913 mL
40 mM 0.0477 mL 0.2387 mL 0.4774 mL 1.1935 mL
50 mM 0.0382 mL 0.1910 mL 0.3819 mL 0.9548 mL
60 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7956 mL
80 mM 0.0239 mL 0.1193 mL 0.2387 mL 0.5967 mL
100 mM 0.0191 mL 0.0955 mL 0.1910 mL 0.4774 mL
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CHI-KAT8i5 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:

CHI-KAT8i5Histone AcetyltransferaseApoptosisHATsHATESCCColon cancerMelanomaGastric cancerNon-small cell adenocarcinomaLiver cancerPDXAnti-tumor.Inhibitorinhibitorinhibit

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