2. Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. DNA/RNA Synthesis Ferroptosis Apoptosis Reactive Oxygen Species (ROS)
  4. KY386

KY386 is a DHX33 helicase inhibitor with an IC50 of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe2+, and decreases the level of GSH in cancer cells. KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma.

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KY386

KY386 Chemical Structure

CAS No. : 2787598-01-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

KY386 is a DHX33 helicase inhibitor with an IC50 of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe2+, and decreases the level of GSH in cancer cells. KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma[1][2].

IC50 & Target

Helicase

 

Cellular Effect
Cell Line Type Value Description References
U-251 IC50
0.02 μM
Compound: IV-a; KY386
Antiproliferative activity against human U-251MG cells overexpressing DHX33 assessed as inhibition of cell growth measured after 48 hrs by CCK-8 assay
Antiproliferative activity against human U-251MG cells overexpressing DHX33 assessed as inhibition of cell growth measured after 48 hrs by CCK-8 assay
[PMID: 37838340]
In Vitro

KY386 (0-640 nM; 60 min) potently and selectively inhibits the helicase activity of recombinant wild-type DHX33 protein, with an IC50 of 0.019 μM[1].
KY386 (5 nM-20 μM; 48 h) potently inhibits the viability of U251-MG cancer cells overexpressing DHX33, with an IC50 of 0.02 μM[1].
KY386 (72 h) exhibits broad nanomolar anticancer activity against most of the DU145, HCT-116, HepG2, K-562, LoVo, MDA-MB-231, MIA PaCa-2, PC-3, SK-BR-3, NCI-H1299, NCI-H1975,
HCC1806, SNU-1, BT549, HCT-15, U-937, A-498, KYSE-150, A549, Daudi, Jurkat T, SNU-387, SW480, Caki-1, SNU-423, CALU-1, COLO 829, T84, U-87MG, NCI-N87, MeWo, HEEC, HGC27 and SGC7901 cells[2].
KY386 (72 h) inhibits the cell viability of human cancer cell lines A875, A375, T24, 5637, SGC7901, HGC27 and SNU668, with IC50 values ranging from 13 nM (A375) to 35 nM (A875)[2].
KY386 (0-500 nM; 24-72 h) potently induces dose- and time-dependent apoptosis in HuH-7 hepatocellular carcinoma cells and HCT116 colorectal cancer cells[2].
KY386 (0-50 nM; 4-24 h) induces dose- and time-dependent increases in intracellular ROS levels in a variety of human cancer cell lines, including HGC27, 5637, T24, A375, A875, DU145, PC3 and SNU668[2].
KY386 (0-40 nM; 8-16 h) induces a dose- and time-dependent decrease in intracellular GSH levels in HGC27 gastric cancer cells[2].
KY386 (0-60 nM; 8-16 h) induces dose- and time-dependent increases in intracellular LPO levels in HGC27, 5637, DU145 and A875 human cancer cells[2].
KY386 (0-60 nM; 16 h) induces a dose-dependent increase in intracellular Fe2+ levels in 5637, HGC27, DU145, PC3 and SNU668 human cancer cells[2].
KY386 (0-50 nM; 24 h) reduces the protein expression of lipid metabolism-related factors FADS1, FADS2 and SCD1 in human cancer cell lines HGC27, 5637, A875, PC-3 and SNU668, while exerting minimal effects on ferroptosis-related factors GPX4, SLC3A2 and SLC7A11[2].
KY386 (0-40 nM; 0-8 h) induces dose-dependent downregulation of FADS1, FADS2 and SCD1 mRNA levels in human cancer cell lines A875, A375, HGC27, T24 and DU145[2].

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

KY386 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: U251-MG DHX33-overexpressing glioblastoma cancer cells
Concentration: 5 nM, 10 nM, 25 nM, 50 nM, 100 nM, 250
nM, 500 nM, 1000 nM, 2000 nM, 5000 nM, 10 μM or 20 μM
Incubation Time: 48 h
Result: Exhibited potent cytotoxicity against U251-MG cells, with an IC50 of 0.02 μM (20 nM).
Demonstrated moderate metabolic stability with an intrinsic clearance (CLint) of 22.4 mL/min/mg in human liver microsomes.

Apoptosis Analysis[2]

Cell Line: HuH-7, HCT116, HGC27, and DU145 human cancer cell lines
Concentration: 20 nM, 100 nM, 500 nM (HuH-7, HCT116); 50 nM, 100 nM, 500 nM (HGC27, DU145, 24 h); 100 nM (HGC27, DU145, 48 h)
Incubation Time: 48 h, 72 h (HuH-7, HCT116); 24 h, 48 h (HGC27, DU145)
Result: Induced apoptosis in a dose- and time-dependent manner in HuH-7 and HCT116 cells.
Did not effectively induce apoptosis in HGC27 and DU145 cells, even with increased dose or treatment time.

Western Blot Analysis[2]

Cell Line: HGC27, 5637, A875, PC-3, and SNU668 human cancer cell lines
Concentration: 20 nM, 40 nM (HGC27, SNU668); 10 nM, 20 nM, 40 nM (5637); 30 nM, 40 nM (A875); 30 nM, 50 nM (PC-3)
Incubation Time: 24 h
Result: Reduced protein expression of FADS1, FADS2, and SCD1 in all tested cancer cell lines.
Had limited effect on GPX4, SLC3A2, and SLC7A11 expression.

Real Time qPCR[2]

Cell Line: A875, A375, HGC27, T24, and DU145 human cancer cell lines
Concentration: 40 nM (A875, A375, HGC27, DU145); 20 nM, 40 nM (T24, DU145)
Incubation Time: 4 h, 6 h, 8 h (A875, A375, HGC27, DU145); 6 h (T24, DU145)
Result: Significantly reduced mRNA levels of FADS1, FADS2, and SCD1 in a time- and dose-dependent manner in all tested cancer cell lines, with statistically significant decreases observed at all specified time points and doses.
In Vivo

KY386 (25-45 mg/kg; i.p.; twice daily for 2 days + three times daily for 1 day; total 7 days) dose-dependently inhibits the growth of SNU668 gastric cancer xenografts in nude mice[2].
KY386 (15-35 mg/kg on days 0-8, 25-45 mg/kg on days 9-20; i.p.; 2 times daily for 2 consecutive days + 3 times daily for 1 consecutive day; total duration of 21 days) significantly inhibits the growth of RASG12D-mutated colon cancer patient-derived xenografts in nude mice[2].

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

Animal Model: Nude mice (female, 5-week old)[2]
Dosage: 25 mg/kg; 35 mg/kg; 45 mg/kg
Administration: i.p.; BID×2 + TID×1; 7 days
Result: Inhibited tumor growth in a dose-dependent manner.
Reduced mean tumor volumes compared to vehicle controls at 21 days post-treatment, with the 45 mg/kg dose showing the greatest inhibition.
Caused no significant reduction in mouse body weight, indicating minimal toxicity.
Animal Model: Nude mice (female, 8-week old)[2]
Dosage: 15 mg/kg (Days 0-8) then 25 mg/kg (Days 9-20); 25 mg/kg (Days 0-8) then 35 mg/kg (Days 9-20); 35 mg/kg (Days 0-8) then 45 mg/kg (Days 9-20)
Administration: i.p.; BID×2 + TID×1; 21 days
Result: Significantly inhibited tumor growth in the RAS G12D mutant colon cancer PDX model.
Reduced mean tumor volumes compared to vehicle controls at 21 days post-treatment.
Caused no significant reduction in mouse body weight, indicating minimal toxicity.
Molecular Weight

405.47

Formula

C21H19N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C2N=C(NC2=C1)NC(C3=C(N(C(C)=C3)C4=C(C=C(S4)C)C#N)C)=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 : 100 mg/mL (246.63 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 2.4663 mL 12.3314 mL 24.6627 mL
5 mM 0.4933 mL 2.4663 mL 4.9325 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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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:

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 2.4663 mL 12.3314 mL 24.6627 mL 61.6568 mL
5 mM 0.4933 mL 2.4663 mL 4.9325 mL 12.3314 mL
10 mM 0.2466 mL 1.2331 mL 2.4663 mL 6.1657 mL
15 mM 0.1644 mL 0.8221 mL 1.6442 mL 4.1105 mL
20 mM 0.1233 mL 0.6166 mL 1.2331 mL 3.0828 mL
25 mM 0.0987 mL 0.4933 mL 0.9865 mL 2.4663 mL
30 mM 0.0822 mL 0.4110 mL 0.8221 mL 2.0552 mL
40 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
50 mM 0.0493 mL 0.2466 mL 0.4933 mL 1.2331 mL
60 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
80 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
100 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6166 mL
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KY386 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:

KY3862787598-01-8KY 386KY-386DNA/RNA SynthesisFerroptosisApoptosisReactive Oxygen Species (ROS)DHX33 helicase inhibitorferroptosisapoptosisU251-MG cellsA875 cellsA375 cellsT24 cells5637 cellsSGC7901 cellsHGC27 cellsSNU668 cellsliver cancerlung cancerpancreatic cancercolorectal cancergastric cancerbreast cancerleukemiarenal cancerprostate canceresophageal cancercervical cancerbrain cancer (glioblastoma)melanomaNude miceInhibitorinhibitorinhibit

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