1. Cell Cycle/DNA Damage
  2. IRE1
  3. MKC8866

MKC8866 

Cat. No.: HY-104040 Purity: 98.38%
Handling Instructions

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits DTT-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth .

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

MKC8866 Chemical Structure

MKC8866 Chemical Structure

CAS No. : 1338934-59-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits DTT-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth [2].

IC50 & Target

IC50: 0.29 μM (IRE1 RNase)[1]

In Vitro

MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines[2].
MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase[2].
MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells[1].
MKC8866 (20 μM; 72 hours) is sufficient to completely block paclitaxel-induced expression of XBP1s [1].

Cell Proliferation Assay[2]

Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells
Concentration: 20 μM
Incubation Time: For 6 days
Result: Decreased proliferation of all breast cancer cell lines.

Cell Cycle Analysis[2]

Cell Line: MDA-MB-231, MCF7 and SKBR3 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: Reduced the number of cells entering S phase.

Cell Cycle Analysis[1]

Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cells
Concentration: 0.2, 0.5, 1, 5, 10 μM
Incubation Time: 3 days
Result: Suppressed the viability of all four cell lines in a dose-dependent manner.

Cell Cycle Analysis[2]

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 72  hours
Result: Completely blocked paclitaxel-induced expression of XBP1s.
In Vivo

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-paclitaxel withdrawal[1].

Animal Model: Female athymic nude mice with MDA-MB-231 tumor[1]
Dosage: 300 mg/kg
Administration: Oral; for 28 days
Result: Reduced tumor regrowth post-paclitaxel withdrawal.
Molecular Weight

361.35

Formula

C₁₈H₁₉NO₇

CAS No.

1338934-59-0

SMILES

O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O

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 : 16.67 mg/mL (46.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7674 mL 13.8370 mL 27.6740 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 mL
10 mM 0.2767 mL 1.3837 mL 2.7674 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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MKC8866
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