URMC-099

SKU: orb1301112

Description

URMC-099 is a potent, orally bioavailable, and brain-penetrant small molecule inhibitor targeting mixed-lineage kinases (MLKs) and LRRK2. It is widely used in preclinical research to investigate neuroinflammation, neurodegeneration, and lysosomal function in both cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Metabolism Research, Molecular Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1229582-33-5
• MW: 421.54
• Purity: 99.98% (May vary between batches)
• Formula: C₂₇H₂₇N₅
• SMILES: CN1CCN(Cc2ccc(cc2)-c2cnc3[nH]cc(-c4ccc5[nH]ccc5c4)c3c2)CC1
• Target: LRRK2,VEGFR,ROCK,c-Met/HGFR,Aurora Kinase,MEK,IGF-1R,DNA Alkylation,Autophagy,Trk receptor,MLK,CDK,SGK,Syk,Bcr-Abl,Src
• Solubility: DMSO:75 mg/mL (177.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.74 mM);Ethanol:6 mg/mL (14.23 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  FLT3:4 nM|ERK2:6290 nM|Aurora A:108 nM|JNK1:3280 nM|Abl-1:6.8 nM|ROCK1:1030 nM|LCK:333 nM|SRC:4330 nM|Aurora B:123 nM|SGK1:201 nM|TRKB:217 nM|MLK3:14nM|ROCK2:111 nM|AMPK:1512 nM|Syk:731 nM|p38α:12050 nM|DLK:150 nM|Abl-1 (T315I):3 nM|CYP3A4:16.2 μM|CDK2:1180 nM|FLT1:39 nM|Aurora C:290 nM|SGK:67 nM|ZAP70:5050 nM|MLK1:19nM|TRKA:85 nM|MEKK2:661 nM|CDK1:1125 nM|IGF-1R:307 nM|MLK2:42nM|LRRK2:11 nM|TNF-α:460 nM|IKKβ:257 nM|c-Met:177 nM|IKKα:591 nM
• In Vivo:
  URMC-099 reduces chemotaxis in wild-type neutrophils induced by fMLP in vitro. Moreover, URMC-099 inhibits the release of TNFα in microglia triggered by lipopolysaccharides, as well as the release of cytokines in human monocytes stimulated by HIV-1 Tat. Additionally, URMC-099 prevents the destruction and phagocytosis of cultured neuronal axons by microglia.
• In Vitro:
  URMC-099, administered intraperitoneally (i.p.) at a dosage of 10 mg/kg, demonstrates the ability to reduce the production of inflammatory cytokines within the body, protect neuronal structures, and alter the morphology and ultrastructural response of microglia to exposure to HIV-1 Tat. In mice, URMC-099 exhibits favorable pharmacokinetics and enhanced Central Nervous System (CNS) penetration. Additionally, URMC-099 significantly reduces the infiltration of neutrophils into the peritoneum of wild-type mice in response to fMLP.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNAAlkylation, DNA Alkylation, DLK, cMet, c-Met, cMet/HGFR, CDK2, CDK1, BcrAbl, Autophagy, Aurora A, Aurora B, AuroraKinase, Aurora C, Aurora Kinase, Abl1, IGF-1R, IGF1R, Inhibitor, Insulin Receptor, Lck, HGFR, MEKK2, inhibit, MLK1, MLK2, MLK3, MLKs, Mixed Lineage Kinase, LRRK2, URMC 099, URMC099, URMC-099, VEGFR1/FLT1, TrkA, Trk receptor, Trkreceptor, TrkB, Syk, ROCK1, ROCK2, SGK1, SGK

Compound Identifiers

PubChem CID

54764565