Belumosudil (KD025) | ROCK2 Inhibitor

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CAS No. :	911417-87-3
Formula :	C₂₆H₂₄N₆O₂
M.W :	452.51
SMILES Code :	CC(NC(COC1=CC=CC(C2=NC3=C(C(NC4=CC5=C(NN=C5)C=C4)=N2)C=CC=C3)=C1)=O)C
Synonyms :	SLx-2119; KD025
MDL No. :	MFCD23098791
InChI Key :	GKHIVNAUVKXIIY-UHFFFAOYSA-N
Pubchem ID :	11950170

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302
Precautionary Statements:	P280-P305+P351+P338

Description	Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively.
Target	ROCK2 ROCK2, Ki:41 nM ROCK2, IC50:60 nM

Bone marrow-derived macrophages (BMDM)	10 µM	20 minutes	To investigate the effect of Belumosudil on IL-17-induced STAT3 phosphorylation, results showed that Belumosudil significantly inhibited IL-17-induced STAT3 phosphorylation.	PMC8645924
Human CD4+ T cells	0.1, 0.5, 1, 2.5, 5, 10 μM	1 hour	KD025 down-regulated the secretion of IL-21 and IL-17 in a dose-dependent manner in vitro, with a lesser effect on IFN-γ secretion.	PMC4250132
Human CD4+ T cells	10 μM	1 hour	KD025 treatment significantly reduced the binding of STAT3 and RNA pII to the promoters of IL-21 and IL-17.	PMC4250132
SW1353 cells	2.5 μM		KD025 significantly downregulated the expression levels of MMP3 and MMP13 and promoted ACAN expression in SW1353 cells, indicating its role in alleviating cartilage degeneration by enhancing FUNDC1-PFKP interaction and mitophagy	PMC10727975
Primary Human Chondrocytes (PHCs)	2.5 μM		KD025 significantly decreased the mRNA expression of MMP3, MMP13, and ADAMTS5, but upregulated ACAN expression in PHCs, indicating its role in alleviating cartilage degeneration by enhancing FUNDC1-PFKP interaction and mitophagy	PMC10727975
SLE CD4+ T cells	90μM	4 days	To evaluate the effect of Y27632 on IL-17 and IL-21 production by SLE CD4+ T cells, results showed that Y27632 significantly inhibited the production of IL-17 and IL-21.	PMC5839171
Human umbilical cord CD4+ T cells	90μM	4 days	To evaluate the effect of Y27632 on IL-17A and IL-21 production by human umbilical cord CD4+ T cells, results showed that Y27632 significantly inhibited the production of IL-17A and IL-21.	PMC5839171

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CAS No.: 911417-87-3

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CAS No.: 911417-87-3

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Mice	Thioacetamide (TAA)-induced liver fibrosis model	Oral gavage	100 mg/kg/day	Once daily for 1 week or 6 weeks	To investigate the prophylactic and therapeutic effects of Belumosudil on TAA-induced liver fibrosis, results showed that Belumosudil significantly attenuated liver fibrosis and promoted fibrotic regression.	PMC8645924
Mice	Collagen-induced arthritis model	Intraperitoneal injection	50, 100, 200 mg/kg	Once daily for 28 days	KD025 treatment markedly down-regulated the progression of inflammatory arthritis and reduced the infiltration of immune cells in joints.	PMC4250132
Mice	DMM-induced osteoarthritis model	Oral	100 mg/kg	Once daily for 4 weeks	KD025 significantly alleviated DMM-induced osteoarthritis and cartilage degeneration by enhancing FUNDC1-PFKP interaction and mitophagy	PMC10727975

NCT05567406	Chronic Graft Versus Host Dise... More >>ase Less <<	PHASE2	RECRUITING	2025-08-27	Nicklaus Children's Hospital- ... More >>Site Number : 129, Miami, Florida, 33155, United States\|University of Maryland School of Medicine - Baltimore- Site Number : 128, Baltimore, Maryland, 21201, United States\|Harvard Medical School - Massachusetts General Hospital (MGH) - Medical Practice Evaluation Center (MPEC)- Site Number : 002, Boston, Massachusetts, 02114, United States\|Dana-Farber Cancer Institute- Site Number : 004, Boston, Massachusetts, 02215, United States\|Washington University- Site Number : 125, Saint Louis, Missouri, 63110, United States\|Westchester Medical Center- Site Number : 130, Valhalla, New York, 10595, United States\|Texas Oncology - Dallas - Worth Street- Site Number : 126, Dallas, Texas, 75246, United States Less <<
NCT02317627	Psoriasis Vulgaris	PHASE2	COMPLETED	2025-03-16	Arrowhead Health Centers, Glen... More >>dale, Arizona, 85306, United States\|Southern California Dermatology, Inc., Santa Ana, California, 92701, United States\|Shondra L. Smith, Lake Charles, Louisiana, 70605, United States\|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States\|Clinical Studies Group, LLC, Henderson, Nevada, 89074, United States\|Icahn School of Medicine at Mount Sinai, New York, New York, 10029, United States\|High Point Clinical Trials Center, High Point, North Carolina, 27265, United States\|Altoona Center for Clinical Research, Duncansville, Pennsylvania, 16635, United States\|Metroplex Clinical Research Center (MCRC), Dallas, Texas, 75231, United States Less <<
NCT04680975	Diffuse Cutaneous Systemic Scl... More >>erosis Less <<	PHASE2	TERMINATED	2022-12-19	University of California, Los ... More >>Angeles Medical Center_Site number 104, Los Angeles, California, 90095, United States\|Yale University School of Medicine_Site number 140, New Haven, Connecticut, 06519, United States\|Northwestern University_Site number 124, Chicago, Illinois, 60611, United States\|Columbia University Medical Center_Site number 086, New York, New York, 10032, United States\|University of Utah_Site number 048, Salt Lake City, Utah, 84132, United States\|Virginia Mason Medical Center_Site number 145, Seattle, Washington, 98101, United States Less <<
NCT02106195	Psoriasis Vulgaris	PHASE2	COMPLETED	2025-09-14	UC Irvine Health, Dept of Derm... More >>atology, Irvine, California, 92697, United States Less <<
NCT06616415	Chronic Graft Versus Host Dise... More >>ase Less <<	PHASE4	RECRUITING	2026-05-04	Investigational Site Number: 1... More >>560001, Beijing, 100045, China\|Investigational Site Number: 1560002, Shanghai, 200127, China Less <<
NCT04166942	Hepatic Impairment	PHASE1	COMPLETED	2022-06-06	Inland Empire Clinical Trials,... More >> LLC-HQ, Rialto, California, 92377, United States\|Clinical Pharmacology of Miami, Miami, Florida, 33014-3616, United States\|Advanced Pharma CR, LLC, Miami, Florida, 33147, United States\|Omega Research Group, Orlando, Florida, 32810, United States\|The Liver Institute, San Antonio, Texas, 78215, United States Less <<

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