Structure of OSS_128167
CAS No.: 887686-02-4
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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.
OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC50s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-cancer, anti-inflammation and anti-viral effects.
Synonyms: OSS-128167; SIRT6-IN-1
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Batch number can be found on the product's label following the word 'Batch'.
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. : | 887686-02-4 |
Formula : | C19H14N2O6 |
M.W : | 366.32 |
SMILES Code : | O=C(O)C1=CC(NC(C2=CC=CC(NC(C3=CC=CO3)=O)=C2)=O)=CC=C1O |
Synonyms : |
OSS-128167; SIRT6-IN-1
|
MDL No. : | MFCD07114226 |
InChI Key : | HTJWLEGCECXGSQ-UHFFFAOYSA-N |
Pubchem ID : | 6496840 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315 |
Precautionary Statements: | P264-P280-P302+P352-P332+P313-P362 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
H9c2 cells | 20 and 50 µM | 1 hour | To evaluate the effects of OSS-128167 on HG-induced fibrosis and apoptosis in H9c2 cells. Results showed that OSS-128167 significantly increased the expression of fibrotic markers COL-1 and TGF-β, and apoptotic proteins Bax and cle-PARP, while decreasing Bcl-2 expression. | PMC7986000 |
RAW264.7 cells | 200 μM | 24 hours | Inhibition of SIRT6 activity promotes M1 macrophage polarization and suppresses M2 polarization | PMC8672560 |
Bone marrow-derived macrophages (BMDM) | 200 μM | 24 hours | Inhibition of SIRT6 activity reduces migration and phagocytosis capacity of macrophages | PMC8672560 |
BV2 cells | 20 µM | 24 hours | CAPE pretreatment reduces ROS generation and promotes M1 to M2 microglia polarization via activating the Sirt6/Nrf2 pathway in H2O2-induced BV2 cells.But this effect could be significantly inhibited by OSS_128167. | PMC10045012 |
CD38+ NK cells | 50 μM | 24 hours | C3G significantly increased Sirtuin 6 (Sirt6) expression and TNF-α level, and decreased natural killer group 2D (NKG2D) expression and IFN-γ level | PMC6819496 |
H9c2 cells | 100 μM | 24 hours | OSS_128167 inhibited H9c2 cell proliferation and promoted apoptosis, while increasing ROS, SA-β-galactosidase, and HK2 levels and decreasing TERT expression. | PMC9792202 |
Human podocytes | 100 μM | 24 hours | Inhibit Sirt6 expression, exacerbate high glucose-induced podocyte cytoskeletal remodeling and apoptosis | PMC11463017 |
HepG2-NTCP cells | 100 µM | 3 days | To evaluate the antiviral effect of OSS_128167 on HBV transcription and replication. Results showed that OSS_128167 significantly reduced the levels of HBV core DNA and 3.5-Kb RNA, and inhibited the secretion of HBsAg and HBeAg. | PMC6823301 |
HepG2.2.15 cells | 100 µM | 3 days | To evaluate the antiviral effect of OSS_128167 on HBV transcription and replication. Results showed that OSS_128167 significantly reduced the levels of HBV core DNA and 3.5-Kb RNA, and inhibited the secretion of HBsAg and HBeAg. | PMC6823301 |
Primary DLBCL cells | 80 µM | 48 hours | To evaluate the effect of OSS_128167 on apoptosis in primary DLBCL cells, results showed significant increase in apoptosis rate | PMC7382040 |
LY8 cells | 100 µM | 48 hours | To evaluate the effect of OSS_128167 on DLBCL cell viability, results showed significant reduction in cell viability after 48 hours | PMC7382040 |
LY1 cells | 100 μM | 48 hours | To evaluate the effect of OSS_128167 on DLBCL cell viability, results showed significant reduction in cell viability after 48 hours | PMC7382040 |
Mononuclear cells (MNCs) | 50 μM | 48 hours | C3G stimulated MNCs to increase IL-2 and IL-10 production and the Treg cell proportion, and it decreased IL-6 and IFN-γ production and the CD38+ NK cell proportion | PMC6819496 |
RA synovial fibroblasts (RASFs) | 50 μM | C3G significantly increased RASF apoptosis and decreased RASF proliferation and IL-6 production in the culture medium | PMC6819496 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | Acute severe asthma (ASA) and chronic severe asthma (CSA) models | Intraperitoneal injection | 10 mg/kg | Administered 2 h before HDM/LPS challenge | To evaluate the effect of OSS_128167 on airway inflammation and remodeling, results showed that OSS_128167 significantly attenuated airway inflammation and remodeling. | PMC10746710 |
BALB/c nude mice | MDA-MB-231 tumor model | Intraperitoneal injection | 20 and 40 mg/kg | Once daily for 2 weeks | To evaluate the anti-tumor effect of icariin in vivo, results showed that icariin significantly inhibited the growth of MDA-MB-231 tumors. | PMC7648025 |
C57BL/6 mice | Streptozotocin (STZ)-induced type 1 diabetic cardiomyopathy model | Oral gavage | 20 or 50 mg/kg | Every other day for 16 weeks | To evaluate the effects of OSS-128167 on diabetic cardiomyopathy. Results showed that OSS-128167 aggravated diabetes-induced myocardial fibrosis and apoptosis, increased the expression of inflammatory factor TNF-α and oxidative stress levels. | PMC7986000 |
Sprague Dawley (SD) rats | Bovine type II collagen-induced arthritis (CIA) | Tail vein injection | 25 mg/kg | Twice per week for six consecutive administrations | C3G injection significantly alleviated CIA, increased IL-10 level and Treg cell proportion, and decreased IL-6 and IFN-γ levels and CD38+ NK cell proportion | PMC6819496 |
HBV transgenic mice | HBV transgenic mouse model | Intraperitoneal injection | 50 mg/kg | Every 4 days for 12 days | To evaluate the antiviral effect of OSS_128167 in vivo. Results showed that OSS_128167 significantly reduced the levels of HBV DNA, HBsAg, and HBeAg in serum, and inhibited the expression of intrahepatic HBV DNA and RNA. | PMC6823301 |
C57BL/6 male mice | LPS-induced ARDS model | Intraperitoneal injection | 80 mg/kg | Single dose, lasting 24 hours | To investigate the effect of OSS_128167 on LPS-induced ARDS. Results showed that OSS_128167 significantly accelerated LPS-induced loss of tight junction proteins, lung inflammation, and apoptosis, and activated the ERK1/2 pathway while inhibiting lung autophagy. | PMC10110478 |
SCID beige mice | DLBCL xenograft model | Intraperitoneal injection | 80 mg/kg | Every 2 days for 2 weeks | To evaluate the effect of OSS_128167 on tumor growth in DLBCL xenograft model, results showed significant suppression of tumor growth | PMC7382040 |
Tags: OSS_128167 | Sirtuin | Hepatitis B virus | SIRT6 | deacetylase | H3K9 | acetylation | GLUT-1 | TNF-α | chemosensitization | PPARα | SIRT6 inhibitor | sirtuin 6 | SIRT1 inhibitor | SIRT2 inhibitor | sirtuin 1 | sirtuin 2 | 887686-02-4
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Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
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P310 | Immediately call a POISON CENTER or doctor/physician. |
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P322 | |
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P374 | Fight fire with normal precautions from a reasonable distance. |
P376 | Stop leak if safe to do so. Oxidising gases (section 2.4) 1 |
P377 | Leaking gas fire: Do not extinguish, unless leak can be stopped safely. |
P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
P390 | Absorb spillage to prevent material damage. |
P391 | Collect spillage. Hazardous to the aquatic environment |
P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
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. |
P370 + P378 | In case of fire: |
P370 + P380 | In case of fire: Evacuate area. |
P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
P371 + P380 + P375 | In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion. |
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P413 | |
P420 | Store away from other materials. |
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P403 + P233 | Store in a well-ventilated place. Keep container tightly closed. |
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P410 + P403 | Protect from sunlight. Store in a well-ventilated place. |
P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
Disposal | |
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Physical hazards | |
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H200 | Unstable explosive |
H201 | Explosive; mass explosion hazard |
H202 | Explosive; severe projection hazard |
H203 | Explosive; fire, blast or projection hazard |
H204 | Fire or projection hazard |
H205 | May mass explode in fire |
H220 | Extremely flammable gas |
H221 | Flammable gas |
H222 | Extremely flammable aerosol |
H223 | Flammable aerosol |
H224 | Extremely flammable liquid and vapour |
H225 | Highly flammable liquid and vapour |
H226 | Flammable liquid and vapour |
H227 | Combustible liquid |
H228 | Flammable solid |
H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
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 |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
H280 | Contains gas under pressure; may explode if heated |
H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
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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