Structure of GSK343
CAS No.: 1346704-33-3
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
GSK343 emerges as an exceptionally potent and selective inhibitor of EZH2, boasting an IC50 of 4 nM.
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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 1346704-33-3 |
Formula : | C31H39N7O2 |
M.W : | 541.69 |
SMILES Code : | O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O |
MDL No. : | MFCD25563250 |
InChI Key : | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
Pubchem ID : | 71268957 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
mouse oocytes | 1 µM | 14 hours | GSK343 treatment did not affect oocyte meiotic maturation but reduced the level of H3K27me3. | PMC5027481 |
YB5 cells | 1 µM | 96 hours | To study the effect of GSK343 on gene expression, it was found to affect only 1.2% of the transcriptome and preferentially targets genes marked with H3K27me3. | PMC5243171 |
MCF7 cells | 1 µM | 96 hours | To study the effect of GSK343 on gene expression, it was found to affect only 1.2% of the transcriptome and preferentially targets genes marked with H3K27me3. | PMC5243171 |
HL60 cells | 1 µM | 96 hours | To study the effect of GSK343 on gene expression, it was found to affect only 1.2% of the transcriptome and preferentially targets genes marked with H3K27me3. | PMC5243171 |
SK-HEP-1 cells | 3 μM | 72 hours | GSK343 treatment significantly increased CXCL10 expression and promoted NK cell migration. | PMC8325240 |
PLC/PRF/5 cells | 3 μM | 72 hours | GSK343 treatment significantly increased CXCL10 expression and promoted NK cell migration. | PMC8325240 |
MDA-MB-231 | 2 µM | 2 days | Inhibited TNBC cell proliferation, induced G1 phase cell cycle arrest and cellular senescence | PMC6376470 |
MDA-MB-436 | 2 µM | 2 days | Inhibited TNBC cell proliferation, induced G1 phase cell cycle arrest and cellular senescence | PMC6376470 |
MCF7 | 2 µM | 2 days | Had minimal effect on non-TNBC cell proliferation | PMC6376470 |
Human primary myoblasts | 20 nM, 200 nM, 2 μM | 10 days | To assess the impact of the EZH2 inhibitor GSK343 on myoblast differentiation and fusion, measured by PAX7 and MYHC iμMunocytochemistry, and mitochondrial bioenergetics determined using the Seahorse XF96. Results showed that GSK343 treatment led to an increase in PAX7 expression (P≤0.05), decreased myotube fusion (P= 0.043), and an increase in ATP production (P= 0.008), with alterations in the DNA methylation of genes involved in oxidative phosphorylation and myogenesis. | PMC8818655 |
B16 cells | 10 mg/kg | GSK343 impairs the phagocytosis of EMCDRs by macrophages, thereby inhibiting the tumor-promoting polarization of macrophages. | PMC8899568 | |
SYO-1 cells | 2.5 µM | 72 hours | To evaluate the effect of GSK343 on the PRAME-EZH2 dimer, results showed that the combination treatment (GSK343 and ATRA) significantly disrupted the PRAME-EZH2 dimer in SYO-1 cells. | PMC11569238 |
MoJo cells | 2.5 µM | 72 hours | To evaluate the effect of GSK343 on the PRAME-EZH2 dimer, results showed that the combination treatment (GSK343 and ATRA) significantly disrupted the PRAME-EZH2 dimer in MoJo cells. | PMC11569238 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
mice | C57BL/6 mice | intraperitoneal injection | 10 mg/kg | single injection | GSK343 treatment significantly inhibited tumor growth, and this effect was dependent on NK cell activity. | PMC8325240 |
Nude mice | TNBC xenograft model | Intraperitoneal injection | 80 ng | single dose, lasted for 20 hours | Combination of GSK343 with chemotherapy drug Adriamycin significantly inhibited TNBC tumor growth, inducing cellular senescence and apoptosis | PMC6376470 |
mice | PGRN KO mice | intraperitoneal | 20 mg/kg | 5 days per week for 28 days | After treatment of PGRN KO mice with GSK343, the numbers of iNKT, NKT2, and IL-4+ cells were rescued to the same level as that of WT mice, and PLZF expression and airway hyperresponsiveness were also ameliorated. | PMC9525702 |
mice | B16 melanoma model | subcutaneously | 5 mg/kg | Twice a week for 21 days | GSK343 combined with PD1 monoclonal antibody significantly prolonged the survival of B16 melanoma-bearing mice and reduced the number of nodules in the lung and brain. | PMC8899568 |
CD1 mice | MPTP-induced Parkinson's disease model | Intraperitoneal injection | consecutively for 14 days | GSK343 treatment significantly improved behavioral deficits and reduced the alteration of PD hallmarks. Furthermore, GSK343 administration significantly attenuated the neuroinflammatory state through the modulation of canonical and non-canonical NF-κB/IκBα pathway as well as the cytokines expression and glia activation, also reducing the apoptosis process. | PMC10311910 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.85mL 0.37mL 0.18mL |
9.23mL 1.85mL 0.92mL |
18.46mL 3.69mL 1.85mL |
Tags: GSK343 | GSK 343 | GSK-343 | Histone Methyltransferase | Suppressor of Variegation 3-9 Homolog 1 | SUV39H1 inhibitor | histone methyltransferase inhibitor | H3K9 methylation | H3K9me3 | H3K9 methylation | chromatin remodeling | epigenetic regulation | gene silencing | histone modification | chromatin dynamics | 1346704-33-3
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Code | Phrase |
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P378 | |
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P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
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H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
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Health hazards | |
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H301 | Toxic if swallowed |
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H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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