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Cat. No.: HY-175841

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Tau Protein Phosphorylation-IN-1

Tau Protein Phosphorylation-IN-1 is a tau protein phosphorylation inhibitor that potently protects PC12 cells against Aβ_25–35-induced cytotoxicity (EC₅₀ = 1.93 μM), and can penetrate the blood-brain barrier (BBB).Tau Protein Phosphorylation-IN-1 reverses the hyperphosphorylation of tau, significantly inhibits the expression of certain immune-related cytotoxic factors, suppresses the MAPK and NF-κB signaling pathways, and significantly inhibits the expression of RAGE and the apoptosis factors Bax/Bcl-2, both in vitro and in vivo. Tau Protein Phosphorylation-IN-1 relieves nerve damage, and improves learning and memory in an Alzheimer’s disease (AD) mouse model. Tau Protein Phosphorylation-IN-1 can be used for AD research.

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

CAS No.: 3075165-36-2
Formula: C₃₉H₅₆N₄O₃
Molecular Weight:628.89

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

Tau Protein Phosphorylation-IN-1 Chemical Structure

CAS No.: 3075165-36-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All p38 MAPK Isoforms :

All NF-κB Isoforms :

All Bcl-2 Family Isoforms :

All ERK Isoforms :

All JNK Isoforms :

In Vitro

Tau Protein Phosphorylation-IN-1 (compound B1) (24 h) shows no toxicity in PC12 cells at 30 μM, and shows significant activity against Aβ_25-35 (HY-P0128)-induced cytotoxicity in PC12 cells at 10 μM^[1].
Tau Protein Phosphorylation-IN-1 (2.5-10 μM, 24 h) demonstrates multi-target neuroprotective effects in Aβ_25-35-induced PC12 cells by significantly reducing tau phosphorylation at Thr181, Thr205, and Ser396, suppressing the phosphorylation of MAPKs (p38, ERK, JNK) and NF-κB, reversing the Aβ-induced upregulation of iNOS and COX-2, and modulating the expression of apoptosis-related proteins Bax and Bcl-2 alongside RAGE inhibition^[1].

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

Western Blot Analysis^[1]

Cell Line:

PC12 cells
Concentration:

2.5, 5 and 10 μM
Incubation Time:

24 h
Result:

Decreased phosphorylated tau levels at Thr181, Thr205, and Ser396 sites caused by Aβ_25–35 compared to the model group.
Exhibited stronger inhibition of tau phosphorylation at the Thr181, Thr205, and Ser396 sites than Oleanolic acid (OA)(HY-N0156) or Donepezil (HY-14566) at 10 μM.
Reversed the Aβ_25–35-induced upregulation of iNOS and COX-2 levels.
Significantly inhibited RAGE expression at 5 and 10 μM.
Decreased Bax and Bcl-2 expression compared to the control group.
Inhibited the phosphorylation of p38 MAPK, ERK and JNK, thereby blocking the MAPK signaling pathway.
Reduced the expression of p-NF-κB in Aβ_25–35-induced PC12 cells.

In Vivo

Tau Protein Phosphorylation-IN-1 (2.5, 5 and 10 mg/kg, i.p., daily for 28 days) rescues cognitive deficits, attenuates tau hyperphosphorylation, and suppresses neuroinflammation in an AD mouse model^[1].

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

Animal Model:

Male ICR mice (20-22 g) intracerebroventricularly injected with Aβ₂₅–₃₅ solution (9 nmol/3 μL/mouse) ^[1]
Dosage:

2.5, 5 and 10 mg/kg
Administration:

i.p., daily for 28 days
Result:

Reduced the escape latencies on training days 2-5 compared with the Aβ group in the Morris water maze test.
Increased the number of crossings over the original platform location, in contrast to the significant reduction observed in the Aβ group.
Reversed the Aβ-induced histopathological damage, including irregular neuronal distribution and reduced cell numbers in the hippocampal CA1 and CA3 areas.
Significantly reduced the levels of tau phosphorylation at Thr205, and Ser396 sites, compared with the Aβ group.
Significantly decreased the level of tau phosphorylation at the Thr181 site in the hippocampus, especially in the DG, CA1, and CA3 pyramidal neurons.
Suppressed the Aβ_25-35-induced upregulation of iNOS, COX-2, RAGE, and the Bax/Bcl-2 ratio.
Showed an inhibitory effect on p38 MAPK, ERK, and JNK phosphorylation in Aβ_25-35-induced AD mice.
Inhibited the Aβ_25-35-induced upregulation of NF-κB in a dose-dependent manner.
Caused no histopathological damage in the liver or kidneys at any tested dose (up to 10 mg/kg) over 21 days.

Chemical Information

CAS No. 3075165-36-2
Molecular Weight 628.89
Formula C₃₉H₅₆N₄O₃
SMILES

O=C([C@]12[C@](CC(C)(CC2)C)([H])C3=CC[C@@]([C@@]4([C@@](C(C)([C@H](CC4)O)C)([H])CC5)C)([H])[C@]5(C)[C@@]3(CC1)C)OCCN6C(C7=CC=CC=C7)=NN=N6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liu Z, et al. Discovery of oleanolic acid derivatives that inhibit tau protein phosphorylation and neuroinflammation induced by Aβ25-35 in vitro and in vivo. Bioorg Chem. 2025 Sep;164:108866. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Tau Protein Phosphorylation-IN-1

All p38 MAPK Isoforms

All NF-κB Isoforms

All Bcl-2 Family Isoforms

All ERK Isoforms

All JNK Isoforms