2. PROTAC Neuronal Signaling
  3. PROTACs Tau Protein
  4. C004019

C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: AZD2858 (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))

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

C004019 Chemical Structure

C004019 Chemical Structure

CAS No. : 2417159-57-8

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Based on 1 publication(s) in Google Scholar

C004019 Related Antibodies

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Description

C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: AZD2858 (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))[1]

In Vitro

C004019 (0.01-100 μM; 24 h) does not cause significant changes in the viability of HEK293 cells stably expressing wild-type full-length human tau (HEK293-hTau)[1].
C004019 (0.01-20 μM; 24 h) inhibits the expression of total tau (Tau5) and phosphorylated tau in HEK293-hTau and SH-SY5Y cells[1].

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

C004019 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293-hTau cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM and 20 μM
Incubation Time: 24 h
Result: Induced a concentration-dependent reduction of total tau (Tau5) and tau phosphorylated (p-tau) at multiple AD-related sites (pS214, pS262, pS396, pS404).
In Vivo

C004019 (intracerebroventricular injection; 5 μL; 200 μM; single dose) reduces the level of tau protein in the brains of wild-type and 3xTg-AD mice[1].
C004019 (subcutaneous injection; 3-15 mg/kg; single dose) effectively clears tau protein in the brains of wild-type mice[1].
C004019 (subcutaneous injection; 3 mg/kg; once every 6 days for five times) promotes tau clearance and improves cognitive and synaptic functions in hTau and 3xTg-AD mice[1].

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

Animal Model: hTau transgenic mice aged 12 months old[1]
Dosage: 3 mg/kg
Administration: Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
Result: Significantly reduced total and p-tau levels in the hippocampal extracts.
Reduced both soluble and insoluble tau, more efficiently to the tau in the soluble fraction.
Ameliorated cognitive functions and dentritic plasticity in hTau transgenic mouse model.
Animal Model: 3xTg-AD mice aged 9.5 months old[1]
Dosage: 3 mg/kg
Administration: Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
Result: Remarkably reduced both soluble and insoluble tau levels in hippocampal and cortex extracts, more efficiently to the tau in the soluble fraction.
Significantly reduced T22-positive tau in the soluble fraction.
Improved the cognitive and synaptic functions in 3xTg-AD mice.
Molecular Weight

1035.29

Formula

C49H70N12O9S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCNC(CN(C4=NC(N5CCN(CCC5)C(C)=O)=NC(NCCC6=CC=CS6)=N4)C)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (48.30 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 0.9659 mL 4.8296 mL 9.6591 mL
5 mM 0.1932 mL 0.9659 mL 1.9318 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 (protect from light). 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 Dissolution Calculator
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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 (protect from light). 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 0.9659 mL 4.8296 mL 9.6591 mL 24.1478 mL
5 mM 0.1932 mL 0.9659 mL 1.9318 mL 4.8296 mL
10 mM 0.0966 mL 0.4830 mL 0.9659 mL 2.4148 mL
15 mM 0.0644 mL 0.3220 mL 0.6439 mL 1.6099 mL
20 mM 0.0483 mL 0.2415 mL 0.4830 mL 1.2074 mL
25 mM 0.0386 mL 0.1932 mL 0.3864 mL 0.9659 mL
30 mM 0.0322 mL 0.1610 mL 0.3220 mL 0.8049 mL
40 mM 0.0241 mL 0.1207 mL 0.2415 mL 0.6037 mL
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C004019 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:

C0040192417159-57-8C 004019C-004019PROTACsTau ProteinHEK293SH-SY5Y3xTg-AD micehTau transgenic miceInhibitorinhibitorinhibit

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