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LDN-212854 is an inhibitor of BMP and can inhibit ALK2 with IC50 of 1.3 nM. It is used to prevent heterotopic ossification.
Synonyms: BMP Inhibitor III
4.5
*For Research Use Only !
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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'.
Search for reports by entering the product batch number.
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'.
Search for reports by entering the product batch number.
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'.
CAS No. : | 1432597-26-6 |
Formula : | C25H22N6 |
M.W : | 406.48 |
SMILES Code : | C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2 |
Synonyms : |
BMP Inhibitor III
|
MDL No. : | MFCD28099808 |
InChI Key : | BBDGBGOVJPEFBT-UHFFFAOYSA-N |
Pubchem ID : | 60182388 |
GHS Pictogram: | ![]() |
Signal Word: | Danger |
Hazard Statements: | H301 |
Precautionary Statements: | P301+P310 |
Class: | 6.1 |
UN#: | 2811 |
Packing Group: | Ⅲ |
Target |
|
In Vitro:
Cell Line
| Concentration | Treated Time | Description | Reference |
Huh7 cells | 1 μM | 48 hours | PMC8835914 | |
Hep3B cells | 5 ng/mL | 48 hours | BMP9 promotes cell cycle progression by reducing RNA m6A methylation levels | PMC10816017 |
Huh7 cells | 5 ng/mL | 48 hours | PMC10816017 | |
MT cells | 1 μM | 48 hours | Suppressed HIF-1α/VEGFA expression and VEGFA secretion | PMC8835914 |
Human DIPG cell lines (SU DIPG IV, DIPG007, SF8628) | 0.1 μM to 10 μM | To evaluate the effect of LDN212854 on proliferation of human DIPG cell lines, results showed that ACVR1 mutant cell lines were more sensitive to LDN212854. | PMC6399349 | |
Mesenchymal cells | 750 nM | 12, 24, 48, 72, and 96 hr | Evaluate the effect of LDN-212854 on mesenchymal cell proliferation, results show LDN-212854 significantly reduces cell proliferation | PMC5542633 |
Primary rat OPCs | 0.18 μM | 3 days | To evaluate the effect of LDN-212854 on OPC differentiation in the presence of fibrinogen, results showed that LDN-212854 restored mature oligodendrocyte differentiation and reduced GFAP+ astrocyte formation. | PMC8418337 |
HSG cells | 0.1, 1.0 or 10 nM | 4 days | To investigate the effect of LDN-212854 on BMP6-induced loss of cell membrane water permeability. Results showed that LDN-212854 inhibited BMP6-induced RVD loss in a dose-dependent manner. | PMC7031521 |
HSG cells | 10 or 60 nM | 24 hours | To investigate the effect of LDN-212854 on BMP6-induced loss of cell membrane water permeability. Results showed that LDN-212854 inhibited BMP6-induced RVD loss in a dose-dependent manner. | PMC7031521 |
C2C12 cells | 500 nM | 3 days | To test the inhibitory effect of LDN-212854 on BMP2-induced alkaline phosphatase (ALP) activity, results showed that LDN-212854 significantly suppressed ALP activity. | PMC10998299 |
Human mesenchymal stromal cells (MSCs) | 500 nM | 28 days | To test the effect of LDN-212854 on MSC chondrogenesis in vitro, results showed that LDN-212854 mildly inhibited chondrogenesis but had limited effects on hypertrophy markers. | PMC10998299 |
Bone marrow mononuclear cells (BMMs) | 1 μM | 5 days | LDN-212854 inhibits SMAD1/5/9 phosphorylation, thereby inhibiting osteoclastogenesis in caAcvr1 mutant cells. | PMC6879329 |
In Vivo:
Species
| Animal Model
| Administration | Dosage | Frequency | Description | Reference |
Mouse | Acvr1[R206H]FlEx/+ conditional knock-in mice | Subcutaneous injection | 3 mg/kg | Twice daily for 4 weeks | LDN-212854 effectively suppressed spontaneous joint/ligament HO and injury-triggered intramuscular HO in Acvr1R206H mice, demonstrating selective ACVR1 inhibition abrogates cell-autonomous effects of mutant receptors in tendon and muscle progenitors. | PMC6407419 |
Mice | Ntv-a;p53fl/fl mice | Intraperitoneally | 10 mg/kg (in vitro), 6 mg/kg (in vivo survival study) | Twice daily for 5 consecutive days (in vitro); twice a day until euthanasia endpoints were met (in vivo survival study) | To evaluate the effect of LDN212854 on tumor growth and survival, results showed that LDN212854 significantly prolonged survival. | PMC6399349 |
Mice | Burn/tenotomy model | Intraperitoneal injection | 6 mg/kg | Daily for 6 weeks | Evaluate the effect of LDN-212854 on trauma-induced heterotopic ossification, results show LDN-212854 significantly reduces heterotopic ossification volume | PMC5542633 |
Mice | Chronic MOG 35-55 EAE model and progressive EAE model in non-obese diabetic mice | 14 days (MOG 35-55 EAE) and 30 days (non-obese diabetic EAE) | To evaluate the therapeutic effects of LDN-212854, results showed that LDN-212854 significantly improved clinical scores, reduced fibrinogen deposition and demyelination, and decreased NG2 cell clustering and myelin damage. | PMC8418337 | ||
Mice | C57BL/6.NOD-Aec1Aec2 mouse model | Intraperitoneal injection | 2.5 mg/kg | Once daily for 24 days | To investigate the effect of LDN-212854 on the restoration of salivary gland function in C57BL/6.NOD-Aec1Aec2 mice. Results showed that LDN-212854 treatment significantly increased salivary flow rate and reduced phosphorylation of SMAD1/5/8 and expression of ID3. | PMC7031521 |
NCG mice | HCC xenograft model | Intraperitoneal injection | 6 mg/kg | Twice daily for 10-14 days | LDN-212854 significantly suppressed HCC tumor growth and induced global RNA m6A methylation | PMC10816017 |
NOD/SCID mice | HCC xenograft model | Intraperitoneal injection | 6 mg/kg | Twice daily for 10-14 days | Inhibited HCC tumor growth and angiogenesis | PMC8835914 |
Tags: LDN-212854 | LDN212854 | LDN 212854 | TGF-β Receptor | Transforming growth factor beta receptors | BMP | FOP model | heterotopic ossification | BMP inhibitor | ALK2 inhibitor | ALK1 inhibitor | 1432597-26-6
Precautionary Statements-General | |
Code | Phrase |
P101 | If medical advice is needed,have product container or label at hand. |
P102 | Keep out of reach of children. |
P103 | Read label before use |
Prevention | |
Code | Phrase |
P201 | Obtain special instructions before use. |
P202 | Do not handle until all safety precautions have been read and understood. |
P210 | Keep away from heat/sparks/open flames/hot surfaces. - No smoking. |
P211 | Do not spray on an open flame or other ignition source. |
P220 | Keep/Store away from clothing/combustible materials. |
P221 | Take any precaution to avoid mixing with combustibles |
P222 | Do not allow contact with air. |
P223 | Keep away from any possible contact with water, because of violent reaction and possible flash fire. |
P230 | Keep wetted |
P231 | Handle under inert gas. |
P232 | Protect from moisture. |
P233 | Keep container tightly closed. |
P234 | Keep only in original container. |
P235 | Keep cool |
P240 | Ground/bond container and receiving equipment. |
P241 | Use explosion-proof electrical/ventilating/lighting/equipment. |
P242 | Use only non-sparking tools. |
P243 | Take precautionary measures against static discharge. |
P244 | Keep reduction valves free from grease and oil. |
P250 | Do not subject to grinding/shock/friction. |
P251 | Pressurized container: Do not pierce or burn, even after use. |
P260 | Do not breathe dust/fume/gas/mist/vapours/spray. |
P261 | Avoid breathing dust/fume/gas/mist/vapours/spray. |
P262 | Do not get in eyes, on skin, or on clothing. |
P263 | Avoid contact during pregnancy/while nursing. |
P264 | Wash hands thoroughly after handling. |
P265 | Wash skin thouroughly after handling. |
P270 | Do not eat, drink or smoke when using this product. |
P271 | Use only outdoors or in a well-ventilated area. |
P272 | Contaminated work clothing should not be allowed out of the workplace. |
P273 | Avoid release to the environment. |
P280 | Wear protective gloves/protective clothing/eye protection/face protection. |
P281 | Use personal protective equipment as required. |
P282 | Wear cold insulating gloves/face shield/eye protection. |
P283 | Wear fire/flame resistant/retardant clothing. |
P284 | Wear respiratory protection. |
P285 | In case of inadequate ventilation wear respiratory protection. |
P231 + P232 | Handle under inert gas. Protect from moisture. |
P235 + P410 | Keep cool. Protect from sunlight. |
Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
P308 | IF exposed or concerned: |
P309 | IF exposed or if you feel unwell: |
P310 | Immediately call a POISON CENTER or doctor/physician. |
P311 | Call a POISON CENTER or doctor/physician. |
P312 | Call a POISON CENTER or doctor/physician if you feel unwell. |
P313 | Get medical advice/attention. |
P314 | Get medical advice/attention if you feel unwell. |
P315 | Get immediate medical advice/attention. |
P320 | |
P302 + P352 | IF ON SKIN: wash with plenty of soap and water. |
P321 | |
P322 | |
P330 | Rinse mouth. |
P331 | Do NOT induce vomiting. |
P332 | IF SKIN irritation occurs: |
P333 | If skin irritation or rash occurs: |
P334 | Immerse in cool water/wrap n wet bandages. |
P335 | Brush off loose particles from skin. |
P336 | Thaw frosted parts with lukewarm water. Do not rub affected area. |
P337 | If eye irritation persists: |
P338 | Remove contact lenses, if present and easy to do. Continue rinsing. |
P340 | Remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P342 | If experiencing respiratory symptoms: |
P350 | Gently wash with plenty of soap and water. |
P351 | Rinse cautiously with water for several minutes. |
P352 | Wash with plenty of soap and water. |
P353 | Rinse skin with water/shower. |
P360 | Rinse immediately contaminated clothing and skin with plenty of water before removing clothes. |
P361 | Remove/Take off immediately all contaminated clothing. |
P362 | Take off contaminated clothing and wash before reuse. |
P363 | Wash contaminated clothing before reuse. |
P370 | In case of fire: |
P371 | In case of major fire and large quantities: |
P372 | Explosion risk in case of fire. |
P373 | DO NOT fight fire when fire reaches explosives. |
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. |
Storage | |
Code | Phrase |
P401 | |
P402 | Store in a dry place. |
P403 | Store in a well-ventilated place. |
P404 | Store in a closed container. |
P405 | Store locked up. |
P406 | Store in corrosive resistant/ container with a resistant inner liner. |
P407 | Maintain air gap between stacks/pallets. |
P410 | Protect from sunlight. |
P411 | |
P412 | Do not expose to temperatures exceeding 50 oC/ 122 oF. |
P413 | |
P420 | Store away from other materials. |
P422 | |
P402 + P404 | Store in a dry place. Store in a closed container. |
P403 + P233 | Store in a well-ventilated place. Keep container tightly closed. |
P403 + P235 | Store in a well-ventilated place. Keep cool. |
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 | |
Code | Phrase |
P501 | Dispose of contents/container to ... |
P502 | Refer to manufacturer/supplier for information on recovery/recycling |
Physical hazards | |
Code | Phrase |
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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