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TTK21

MCE China：TTK21

Brand：MedChemExpress (MCE)

Cat. No.HY-116673

CAS：709676-56-2

Purity：99.39%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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.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.

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].

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].

IC50 & Target：CBP/p300

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References：

[1]. Chatterjee S, et al. A novel activator of CBP/p300 acetyltransferases promotes neurogenesis and extends memory duration in adult mice. J Neurosci. 2013;33(26):10698-10712.  [Content Brief]

[2]. Singh A et al. Glucose derived carbon nanosphere (CSP) conjugated TTK21, an activator of the histone acetyltransferases CBP/p300, ameliorates amyloid-beta 1-42 induced deficits in plasticity and associativity in hippocampal CA1 pyramidal neurons. Aging Cell. 2022 Sep;21(9):e13675.  [Content Brief]

[3]. Singh A, et al. Oral administration of a specific p300/CBP Lysine acetyltransferase activator induces synaptic plasticity and repairing spinal cord injury[J]. bioRxiv, 2023: 2023.10. 04.560982.