2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. CDK E1/E2/E3 Enzyme
  4. LO-3-63

LO-3-63, a Ribociclib (HY-15777) analog bearing a truncated fumaramide handle, is a PROTAC-like CDK4/6 degrader. LO-3-63 induces CUL4DCAF16-dependent degradation of CDK4/6 in cells.

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

LO-3-63

LO-3-63 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

LO-3-63 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LO-3-63, a Ribociclib (HY-15777) analog bearing a truncated fumaramide handle, is a PROTAC-like CDK4/6 degrader. LO-3-63 induces CUL4DCAF16-dependent degradation of CDK4/6 in cells[1].

In Vitro

LO-3-63 (1-10 μM, 12-24 h) leads to the proteasome mediated degradation of CDK4/6 in HEK293T cells, an effect that can be attenuated in DCAF16 KO cells[1].

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

LO-3-63 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells (WT, DCAF16 KO)
Concentration: 1, 5, 10 μM
Incubation Time: 12, 24 h
Result: Degraded CDK4/6 in HEK293T cells (WT), an effect that can be attenuated in DCAF16 KO cells.
Molecular Weight

643.14

Formula

C32H35ClN10O3
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(C(/C=C/C(NC5=CC(Cl)=CN=C5)=O)=O)CC4)C=C3)N=C2N1C6CCCC6)N(C)C
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 (155.49 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 1.5549 mL 7.7744 mL 15.5487 mL
5 mM 0.3110 mL 1.5549 mL 3.1097 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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  • 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 1.5549 mL 7.7744 mL 15.5487 mL 38.8718 mL
5 mM 0.3110 mL 1.5549 mL 3.1097 mL 7.7744 mL
10 mM 0.1555 mL 0.7774 mL 1.5549 mL 3.8872 mL
15 mM 0.1037 mL 0.5183 mL 1.0366 mL 2.5915 mL
20 mM 0.0777 mL 0.3887 mL 0.7774 mL 1.9436 mL
25 mM 0.0622 mL 0.3110 mL 0.6219 mL 1.5549 mL
30 mM 0.0518 mL 0.2591 mL 0.5183 mL 1.2957 mL
40 mM 0.0389 mL 0.1944 mL 0.3887 mL 0.9718 mL
50 mM 0.0311 mL 0.1555 mL 0.3110 mL 0.7774 mL
60 mM 0.0259 mL 0.1296 mL 0.2591 mL 0.6479 mL
80 mM 0.0194 mL 0.0972 mL 0.1944 mL 0.4859 mL
100 mM 0.0155 mL 0.0777 mL 0.1555 mL 0.3887 mL
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LO-3-63 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:

LO-3-63CDKE1/E2/E3 EnzymeCyclin dependent kinaseE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseDCAF16HEK293T cellsCDK4/6Inhibitorinhibitorinhibit

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