ChemicalBook > CAS DataBase List > URMC-099

URMC-099

Product Name
URMC-099
CAS No.
1229582-33-5
Chemical Name
URMC-099
Synonyms
RMC099;CS-1776;URMC-099;URMC-099 ，S7343;URMC-099;URMC 099;URMC-099, 10 mM in DMSO;inhibit,MLKs,Autophagy,URMC 099,URMC099,URMC-099,Inhibitor,Mixed Lineage Kinase;3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine;1H-?Pyrrolo[2,?3-?b]?pyridine, 3-?(1H-?indol-?5-?yl)?-?5-?[4-?[(4-?methyl-?1-?piperazinyl)?methyl]?phenyl]?-;3-(1H-indol-5-yl)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine URMC-099
CBNumber
CB62719728
Molecular Formula
C27H27N5
Formula Weight
421.54
MOL File
1229582-33-5.mol
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URMC-099 Property

Density 
1.256±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
form 
solid
pka
13.49±0.40(Predicted)
color 
Off-white
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey
QKKIWEILHCXECO-UHFFFAOYSA-N
SMILES
C12NC=C(C3C=CC4=C(C=3)C=CN4)C1=CC(C1=CC=C(CN3CCN(C)CC3)C=C1)=CN=2
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Safety

HS Code 
2933998090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

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.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19147
Product name
URMC-099
Purity
≥95%
Packaging
5mg
Price
$60
Updated
2024/03/01
Cayman Chemical
Product number
19147
Product name
URMC-099
Purity
≥95%
Packaging
1mg
Price
$29
Updated
2022/04/27
Cayman Chemical
Product number
19147
Product name
URMC-099
Purity
≥95%
Packaging
10mg
Price
$99
Updated
2024/03/01
Cayman Chemical
Product number
19147
Product name
URMC-099
Purity
≥95%
Packaging
25mg
Price
$162
Updated
2024/03/01
TRC
Product number
U842000
Product name
URMC-099
Packaging
1mg
Price
$105
Updated
2021/12/16
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URMC-099 Chemical Properties,Usage,Production

Description

URMC-099 (1229582-33-5) is a potent (IC50 = 14 nM), brain penetrant mixed-lineage kinase 3 inhibitor (MLK3). It also potently inhibits FLT3 (4 nM in vitro, but 560 nM in vivo), LRRK2 (11 nM), and ABL1 (3 nM).1 URMC-099 displayed neuroprotective effects in HIV-associated neurocognitive disorders2 and facilitated microglial amyloid-β degradation and clearance in mouse models.3,4 URMC-099 increased CD8+ T cells in mice and increased the CD8+GZMB+ T cell population in blood mononuclear cells isolated from breast cancer patients.5

Uses

URMC-099 is an orally bioavailable MLK3 inhibitor used in the treatment of Parkinson’s disease and HIV-1 associated neurocognitive disorders.

in vivo

URMC-099 has moderate terminal elimination half-life (t1/2=1.92 h, 2.14 h and 2.72 h for C57 BL/6 mice (10 mg/kg, oral dosing), C57 BL/6 mice (2.5 mg/kg, iv), C57 BL/6 mice (10 mg/kg, iv))[1]. The effect of URMC-099 (URMC099) on tumor formation in vivo is analyzed using a well characterized mouse xenograft model of breast cancer brain metastasis. For these experiments, eGFP8.4 cells are inoculated into the left ventricle of immunodeficient nu/nu mice; animals are then treated with either URMC-099 (10 mg/kg) or vehicle alone, every 12 hours for 20 days. This dose of URMC-099 is chosen because it has been shown to be sufficient to effectively inhibit MLK3 in mice, with good penetration of the blood-brain barrier and potent inhibition of the phosphorylation of Jun N-terminal kinase (JNK) in brain tissue. On day 21 the mice are sacrificed and number of BM is assessed. Fifteen mice are used for each treatment group. BM are detected in 60% of mice, which is consistent with previous studies using this xenograft model by other investigators. URMC-099 treatment significantly (p<0.05, two-tailed t-test) increases the total number of brain metastasis (BM) in mice. For micrometastases, the pattern is similar to that observed for total BM. The number of macrometastases is statistically indistinguishable between mice treated with URMC-099 or vehicle[2].

IC 50

LRRK2: 11 nM (IC50); FLT3: 4 nM (IC50); FLT1: 39 nM (IC50); ABL1 (T315I): 3 nM (IC50); ABL1: 6.8 nM (IC50); SGK: 67 nM (IC50); SGK1: 201 nM (IC50); AurA: 108 nM (IC50); AurB: 123 nM (IC50); AurC: 290 nM (IC50); IKKβ: 257 nM (IC50); IKKα: 591 nM (IC50); TNFα: 460 nM (IC50); ROCK1: 1030 nM (IC50); ROCK2: 111 nM (IC50); CDK1: 1125 nM (IC50); CDK2: 1180 nM (IC50); TRKA: 85 nM (IC50); c-MET: 177 nM (IC50); TRKB: 217 nM (IC50); IGF1R: 307 nM (IC50); LCK: 333 nM (IC50); MEKK2: 661 nM (IC50); SYK: 731 nM (IC50); AMPK: 1512 nM (IC50); JNK1: 3280 nM (IC50); SRC: 4330 nM (IC50); ZAP70: 5050 nM (IC50); ERK2: 6290 nM (IC50); P38α: 12050 nM (IC50); CYP3A4: 16.2 μM (IC50)

References

[1] VAL S. GOODFELLOW*. Discovery, Synthesis, and Characterization of an Orally Bioavailable, Brain Penetrant Inhibitor of Mixed Lineage Kinase 3[J]. Journal of Medicinal Chemistry, 2013, 56 20: 8032-8048. DOI:10.1021/jm401094t
[2] DANIEL F MARKER. The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disorders.[J]. Journal of Neuroscience, 2013, 33 24: 9998-10010. DOI:10.1523/jneurosci.0598-13.2013
[3] WEIGUO DONG. The mixed-lineage kinase 3 inhibitor URMC-099 facilitates microglial amyloid-β degradation.[J]. Journal of Neuroinflammation, 2016: 184. DOI:10.1186/s12974-016-0646-z
[4] TOMOMI KIYOTA. URMC-099 facilitates amyloid-β clearance in a murine model of Alzheimer’s disease.[J]. Journal of Neuroinflammation, 2018: 137. DOI:10.1186/s12974-018-1172-y
[5] SANDEEP KUMAR. Mixed lineage kinase 3 inhibition induces T cell activation and cytotoxicity.[J]. ACS Catalysis , 2020: 7961-7970. DOI:10.1073/pnas.1921325117

URMC-099 Preparation Products And Raw materials

Raw materials

Preparation Products

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URMC-099 Suppliers

China 100 United Kingdom 1 United States 14 Global 115
Nanjing XiZe Biotechnology CO., Ltd.
Tel
025-58362220 0086-15250997978
Fax
025-58362220
Email
sale@njxizebio.com
Country
China
ProdList
4855
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Tongling HengYou Biotechnology Co., Ltd.
Tel
021-50426030 13856289449
Fax
021-50426030
Email
2630597085@qq.com
Country
China
ProdList
1889
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55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
984
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55
ShangHai Angti Biotechnology Co., Ltd.
Tel
13764913901
Fax
-
Email
info@angtibio.com
Country
China
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4985
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55

1229582-33-5, URMC-099Related Search:

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  • 3-(1H-indol-5-yl)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine URMC-099
  • URMC-099
  • 3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine
  • 1H-?Pyrrolo[2,?3-?b]?pyridine, 3-?(1H-?indol-?5-?yl)?-?5-?[4-?[(4-?methyl-?1-?piperazinyl)?methyl]?phenyl]?-
  • CS-1776
  • URMC-099;URMC 099
  • RMC099
  • inhibit,MLKs,Autophagy,URMC 099,URMC099,URMC-099,Inhibitor,Mixed Lineage Kinase
  • URMC-099, 10 mM in DMSO
  • URMC-099 ，S7343
  • 1229582-33-5
  • C27H27N5
  • Inhibitors
  • api