Synonym
Belumosudil free base; KD 025; KD-025; KD025; WHO11343; WHO-11343; WHO 11343; SLx 2119; SLx2119; SLx-2119;
IUPAC/Chemical Name
2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide
InChi Key
GKHIVNAUVKXIIY-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31)
SMILES Code
O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
SLx-2119 is a selective inhibitor of ROCK with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively.
In vitro activity:
SLx-2119 has potential as a combination therapy with antineoplastic drugs for leukemia patients with ATP-binding cassette subfamily G member 2 (ABCG2)-mediated multidrug resistance. ABCG2 overexpression is linked to multidrug resistance in leukemia cells. SLx-2119 enhanced the effectiveness of antineoplastic drugs in ABCG2-overexpressing leukemia cells, inhibited drug efflux, and did not affect ABCG2 protein levels or location.
Reference: Oncol Lett. 2020 Dec;20(6):309. https://pubmed.ncbi.nlm.nih.gov/33093918/
In vivo activity:
Treating arteries with SLX-2119 significantly restored endothelial function in both male and female mice, regardless of strain (FVB/NJ or C57BL/6J). Ang II-induced endothelial dysfunction was observed in all groups but was effectively reversed by inhibiting ROCK2 with SLX-2119. These findings suggest that ROCK2 plays a crucial role in Ang II-induced endothelial dysfunction across sexes and mouse strains with varying susceptibilities to vascular disease.
Reference: Physiol Rep. 2022 Jun;10(11):e15336. https://pubmed.ncbi.nlm.nih.gov/35681278/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
48.0 |
106.10 |
| DMF |
30.0 |
66.30 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
452.52
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Jing W, Zhang X, Chen R, Ye X, Zhou M, Li W, Yan W, Xuyun X, Peng J. KD025, an anti-adipocyte differentiation drug, enhances the efficacy of conventional chemotherapeutic drugs in ABCG2-overexpressing leukemia cells. Oncol Lett. 2020 Dec;20(6):309. doi: 10.3892/ol.2020.12172. Epub 2020 Sep 30. PMID: 33093918; PMCID: PMC7573885.
2. Diep DTV, Duong KHM, Choi H, Jun HS, Chun KH. KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells. Adipocyte. 2019 Dec;8(1):114-124. doi: 10.1080/21623945.2019.1590929. Epub 2019 Mar 23. PMID: 30860936; PMCID: PMC6768280.
3. Kinzenbaw DA, Langmack L, Faraci FM. Angiotensin II-induced endothelial dysfunction: Impact of sex, genetic background, and rho kinase. Physiol Rep. 2022 Jun;10(11):e15336. doi: 10.14814/phy2.15336. PMID: 35681278; PMCID: PMC9184751.
4. Wei L, Surma M, Yang Y, Tersey S, Shi J. ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice. FASEB J. 2020 Jan;34(1):474-493. doi: 10.1096/fj.201901174RR. Epub 2019 Nov 25. PMID: 31914704; PMCID: PMC6956740.
In vitro protocol:
1. Jing W, Zhang X, Chen R, Ye X, Zhou M, Li W, Yan W, Xuyun X, Peng J. KD025, an anti-adipocyte differentiation drug, enhances the efficacy of conventional chemotherapeutic drugs in ABCG2-overexpressing leukemia cells. Oncol Lett. 2020 Dec;20(6):309. doi: 10.3892/ol.2020.12172. Epub 2020 Sep 30. PMID: 33093918; PMCID: PMC7573885.
2. Diep DTV, Duong KHM, Choi H, Jun HS, Chun KH. KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells. Adipocyte. 2019 Dec;8(1):114-124. doi: 10.1080/21623945.2019.1590929. Epub 2019 Mar 23. PMID: 30860936; PMCID: PMC6768280.
In vivo protocol:
1. Kinzenbaw DA, Langmack L, Faraci FM. Angiotensin II-induced endothelial dysfunction: Impact of sex, genetic background, and rho kinase. Physiol Rep. 2022 Jun;10(11):e15336. doi: 10.14814/phy2.15336. PMID: 35681278; PMCID: PMC9184751.
2. Wei L, Surma M, Yang Y, Tersey S, Shi J. ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice. FASEB J. 2020 Jan;34(1):474-493. doi: 10.1096/fj.201901174RR. Epub 2019 Nov 25. PMID: 31914704; PMCID: PMC6956740.
1: Lee JH, Zheng Y, von Bornstadt D, Wei Y, Balcioglu A, Daneshmand A, Yalcin N,
Yu E, Herisson F, Atalay YB, Kim MH, Ahn YJ, Balkaya M, Sweetnam P, Schueller O,
Poyurovsky MV, Kim HH, Lo EH, Furie KL, Ayata C. Selective ROCK2 Inhibition In
Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. PubMed
PMID: 24466563; PubMed Central PMCID: PMC3900310.
2: Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, McGonigle S,
Paradise E, Sweetnam P, Fink LM, Vozenin-Brotons MC, Hauer-Jensen M. Comparative
gene expression profiling in three primary human cell lines after treatment with
a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis. 2008
Oct;19(7):709-18. doi: 10.1097/MBC.0b013e32830b2891. PubMed PMID: 18832915;
PubMed Central PMCID: PMC2713681.
