BML-275
- Product Name
- BML-275
- CAS No.
- 1219168-18-9
- Chemical Name
- BML-275
- Synonyms
- CS-1883;Dorsomorph;BML-275(2HCL);Compound C 2HCl;Dorsomorphin HCl;BML-275,Compound C;Nutlin-3a (Rebemadlin);BML-275 dihydrochloride;Dorsomorphin-2HCl BML-275;BML-275 Dorsomorphin 2HCL
- CBNumber
- CB72614842
- Molecular Formula
- C24H27Cl2N5O
- Formula Weight
- 472.41008
- MOL File
- 1219168-18-9.mol
BML-275 Property
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- insoluble in EtOH; insoluble in H2O; ≥11.34 mg/mL in 0.9% NS ; ≥39.93 mg/mL in DMSO:H2O=2:1 ; ≥5.91 mg/mL in DMSO
- form
- Light yellow powder solid.
- color
- Yellow
- Stability:
- Hygroscopic
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 21207
- Product name
- Dorsomorphin (hydrochloride)
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 21207
- Product name
- Dorsomorphin (hydrochloride)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 21207
- Product name
- Dorsomorphin (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $153
- Updated
- 2024/03/01
- Product number
- 21207
- Product name
- Dorsomorphin (hydrochloride)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $343
- Updated
- 2024/03/01
- Product number
- D534910
- Product name
- DorsomorphinDihydrochloride
- Packaging
- 50mg
- Price
- $425
- Updated
- 2021/12/16
BML-275 Chemical Properties,Usage,Production
Description
Dorsomorphin (hydrochloride) is a potent, reversible inhibitor of AMP kinase (AMPK; Ki = 109 nM) that does not exhibit significant activity on structurally related kinases, including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin can also dose-dependently inhibit the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK6). Independent of AMPK inhibition, dorsomorphin, at 10 μM, has additionally been shown to downregulate the Akt/mTOR pathway to induce autophagy in U251 human glioma cells.
Uses
Dorsomorphin is an AMP-activated kinase (AMPK) inhibitor. Dorsomorphin selectively inhibits the bone morphogenetic protein (BMP) type I receptors ALK2, ALK3 and ALK6 and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. Dorsomorphin has shown to increase cisplatin-induced apoptosis, which was associated with hyper-induction of the tumor suppressor p53.
in vivo
Dorsomorphin (compound C; 10 mg/kg, intravenously once) dihydrochloride treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice[3].
Dorsomorphin (0.2 mg/kg, i.v., 30 min before LPS injection) dihydrochloride reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta[4].
Dorsomorphin (25 mg/kg; i.p. injection, in male BALB/c mice) dihydrochloride treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only[5].
| Animal Model: | Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin[3]. |
| Dosage: | 10 mg/kg. |
| Administration: | Intravenously once. |
| Result: | Led to a 60% increase in total serum iron concentrations. Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice. |
| Animal Model: | Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g)[4]. |
| Dosage: | 0.2 mg/kg. |
| Administration: | I.V., 30 min before LPS injection. |
| Result: | Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta. |
| Animal Model: | Male BALB/c mice at 6-7 weeks of age weighing 20-22 g[5] |
| Dosage: | 25 mg/kg |
| Administration: | Injection i.p.; 60 min before LPS challenge |
| Result: | Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only. |
IC 50
AMPK: 109 nM (Ki); ACVR1; BMPR1A; ALK6; Autophagy
storage
Room temperature (desiccate)
References
[1] ZHOU G, MYERS R W, LI Y, et al. Role of AMP-activated protein kinase in mechanism of metformin action.[J]. The Journal of clinical investigation, 2001, 1 1: 0. DOI: 10.1172/jci13505
[2] PAUL B YU. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism[J]. Nature chemical biology, 2007, 4 1: 33-41. DOI: 10.1038/nchembio.2007.54
[3] LJUBICA VUCICEVIC. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway.[J]. Autophagy, 2011, 7 1: 40-50. DOI: 10.4161/auto.7.1.13883
BML-275 Preparation Products And Raw materials
Raw materials
Preparation Products
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