LM22B-10 is a TrkB/TrkC neurotrophic factor receptor activator that induces the activation of TrkB, TrkC, AKT, and ERK in vivo and in vitro. The maximum neurotrophic survival activity of LM22B-10 was higher than that of BDNF (53 ± 7.2% higher than BDNF at 0.7 nM) and NT-3 (91 ± 8.6% higher than NT-3 at 0.7 nM), with EC50 values of 200-300 nM. The pattern of Trk and downstream signalling activation induced by LM22B-10 was different from that of BDNF and NT-3. The mean neurite length induced by LM22B-10 (1,000 nM) was significantly larger, up to 40 µm. LM22B-10 (250-2000 nM) binds TrkB-Fc and TrkC-Fc in a dose-dependent manner. LM22B-10 inhibits the binding of BDNF to TrkB-expressing cells and the binding of NT-3 to TrkC-expressing cells. LM22B-10 promotes cell survival and acts preferentially on TrkB and TrkC. LM22B-10, but not BDNF or NT-3, promotes neuronal growth in an inhibitory environment. LM22B-10 also induces TrkB, TrkC, AKT and ERK activation in cultured hippocampal neurons[1].
LM22B-10 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone marrow macrophages (BMMs)
30 µM
3 days
Evaluate the inhibitory effect of MRL on mitochondrial function
J Transl Med. 2023 Nov 22;21(1):839.
MDA-MB-231 cells
50 µM
48 hours
Reversed the inhibitory effects of HSP20 overexpression on cell proliferation and migration
Oncol Lett. 2022 Nov 3;24(6):462.
Bone marrow macrophages (BMMs)
30 µM
7 days
Evaluate the inhibitory effect of MRL on osteoclast differentiation
J Transl Med. 2023 Nov 22;21(1):839.
NIH-3T3-TrkC cells
10 to 1000 nM
72 to 96 hours
To assess the effect of BD10-2 on the survival of 3T3 cells expressing TrkC, results showed that BD10-2 promoted survival of 3T3-TrkC cells in a dose-dependent manner
Alzheimers Dement. 2024 Jul;20(7):4434-4460.
NIH-3T3-TrkB cells
10 to 1000 nM
72 to 96 hours
To assess the effect of BD10-2 on the survival of 3T3 cells expressing TrkB, results showed that BD10-2 promoted survival of 3T3-TrkB cells in a dose-dependent manner
Alzheimers Dement. 2024 Jul;20(7):4434-4460.
786-O cells
5 mM
LM22B-10, as an ERK activator, combined with miR-133b overexpression, weakened the anticancer effects of miR-133b.
Mol Med Rep. 2020 Jul;22(1):67-76.
LM22B-10 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Ovariectomy-induced osteoporosis model
Intraperitoneal injection
30 mg/kg
Once a week for 6 weeks
Evaluate the therapeutic effect of MRL on osteoporosis
J Transl Med. 2023 Nov 22;21(1):839.
Mice
APPL/S Mice model
Oral gavage
50 mg/kg
5 days/week for 3 months
To evaluate the effect of BD10-2 on memory and synaptic function in APPL/S mice, results showed that BD10-2 significantly improved memory and long-term potentiation (LTP) deficits and restored abnormalities in synapse-related signaling proteins
Alzheimers Dement. 2024 Jul;20(7):4434-4460.
Nude mice
PNI model
Daily administration
50 mg/kg
Once daily for 2 weeks
To confirm the effects of MMP1 knockdown on PNI, results showed that LM22B-10 partially abolished the effects of MMP1 knockdown.
J Clin Lab Anal. 2022 Nov;36(11):e24719
LM22B-10 动物研究
Animal study
LM22B-10 activated TrkB, TrkC, AKT and ERK in C57BL/6J mice at a dose of 0.5 mg/kg. LM22B-10 increased the phosphorylation of TrkB-Y817 and TrkC-Y820 at a dose of 50 mg/kg when administered intraperitoneally. TrkC and increases pre and post synaptic proteins and spine density in aged mice[1].
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