2. Epigenetics
  3. Histone Acetyltransferase
  4. TTK21

TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory.CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function. CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model.

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TTK21 Chemical Structure

TTK21 Chemical Structure

CAS No. : 709676-56-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 152 In-stock
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1 mg USD 69 In-stock
5 mg USD 138 In-stock
10 mg USD 208 In-stock
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Based on 1 publication(s) in Google Scholar

TTK21 Related Antibodies

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Description

TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory[1].CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function[2]. CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model[3].

IC50 & Target[1]

CBP/p300

 

In Vitro

TTK21 (50-275 μM) is able to concentration-dependently activate CBP and p300 acetyltransferases and increase histone acetylation. Effectively activates CBP/p300 activity and increases the acetylation of histone H3 and H4. 100 μM TTK21 can promote the self-acetylation of p300[1].
TTK21 (50-275 μM; 6-24 h) in Hela cells, can't effectively penetrate the cell membrane to enter the cell by itself. However, when combined with carbon nanosphere CSP, it is able to enter SH-SY5Y neuronal cells and significantly increase the acetylation level of histone H3, indicating that the CSP-TTK21 complex has the ability to penetrate the cell membrane[1].
CSP-TTK21 (0.36 µg/ml; 1 h) can restor protein synthesis-dependent long-term potentiation (LTP) damage caused by Aβ (1-42) multimerst[2].

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

TTK21 Related Antibodies

RT-PCR[2]

Cell Line: Rat hippocampal CA1 area slices
Concentration: CSP-TTK21 0.36 µg/ml
Incubation Time: 1 h
Result: CSP-TTK21 upregulated certain genes whose expression was decreased under Aβ(1–42) treatment, such as genes involved in the Wnt signaling pathway. CSP-TTK21 also potentially downregulated genes associated with inflammation, helping to reduce the neuroinflammatory response caused by Aβ(1–42).
In Vivo

CSP-TTK21 (20 mg/kg; i.p.; single dose) can extend the memory duration[1].
CSP-TTK21 (20 mg/kg; p.o; single dose) enhances long-term potentiation comparably to intraperitoneal injection, suggesting effective memory enhancement in Wild-type mice[3].
CSP-TTK21 (10 mg/kg; p.o; weekly) promotes motor recovery after spinal cord injury in rats, and enhances the expression of regeneration-associated genes in the prefrontal cortex and cerebellum following spinal cord injury[3].

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

Animal Model: B57BL/6J male [1]
Dosage: CSP-TTK21; 20 mg/kg; single dose
Administration: i.p.
Result: Increased histone acetylation significantly in the hippocampus and frontal cortex. CSP-TTK21 crossed the blood-brain barrier and was primarily detected in the brain, liver, and spleen. It promoted differentiation of newly generated neurons in the dentate gyrus.
Mice with CSP-TTK21 displayed a persistent memory of the platform location in a Morris water maze task for a longer period compared to controls, demonstrating enhanced long-term memory.
Animal Model: Wild-type mice [3]
Dosage: CSP-TTK21; 20 mg/kg; single dose
Administration: p.o.
Result: The administered compound crossed the blood-brain barrier, induced histone acetylation specifically H4K12ac and H3K14ac marks in the hippocampus, and did not alter basal synaptic transmission. It was found to enhance long-term potentiation comparably to intraperitoneal injection, suggesting effective memory enhancement through oral delivery.
Animal Model: rats with spinal cord injury[3]
Dosage: CSP-TTK21; 10 mg/kg; weekly
Administration: p.o.
Result: Rats with CSP-TTK21 showed significant improvement in locomotion and rearing activity compared to controls. Histone acetylation was notably increased in the spinal cord, suggesting enhanced gene expression linked to regeneration and functional recovery. Enhanced histone acetylation levels (H4K12ac, H3K27ac, H3K9ac) were observed in the prefrontal cortex and cerebellum of rats with CSP-TTK21, indicating active epigenetic modifications that support neuronal regeneration and functional recovery.
Molecular Weight

357.75

Formula

C17H15ClF3NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C=C1C(F)(F)F)NC(C2=CC=CC=C2OCCC)=O
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 (279.52 mM; ultrasonic and warming and heat to 60°C; 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 2.7952 mL 13.9762 mL 27.9525 mL
5 mM 0.5590 mL 2.7952 mL 5.5905 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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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 (6.99 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
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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 2.7952 mL 13.9762 mL 27.9525 mL 69.8812 mL
5 mM 0.5590 mL 2.7952 mL 5.5905 mL 13.9762 mL
10 mM 0.2795 mL 1.3976 mL 2.7952 mL 6.9881 mL
15 mM 0.1863 mL 0.9317 mL 1.8635 mL 4.6587 mL
20 mM 0.1398 mL 0.6988 mL 1.3976 mL 3.4941 mL
25 mM 0.1118 mL 0.5590 mL 1.1181 mL 2.7952 mL
30 mM 0.0932 mL 0.4659 mL 0.9317 mL 2.3294 mL
40 mM 0.0699 mL 0.3494 mL 0.6988 mL 1.7470 mL
50 mM 0.0559 mL 0.2795 mL 0.5590 mL 1.3976 mL
60 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
80 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8735 mL
100 mM 0.0280 mL 0.1398 mL 0.2795 mL 0.6988 mL
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TTK21 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:

TTK21709676-56-2TTK 21TTK-21Histone AcetyltransferaseHATsHATCBP/p300histone acetyltransferasesblood–brain barriertoxicityneurogenesislong-term memoryCSPspinal injury ratAlzheimer's disease (ADInhibitorinhibitorinhibit

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