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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

Cell Biology, Immunology & Inflammation, Neuroscience

Images & Validation

Key Properties

CAS Number1229582-33-5
MW421.5
Purity>98%
FormulaC27H27N5
SMILESCN1CCN(Cc2ccc(cc2)-c2cnc3[nH]cc(-c4ccc5[nH]ccc5c4)c3c2)CC1
TargetKinase
SolubilitySoluble in DMSO (up to at least 25 mg/ml)

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-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor 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

Similar Products

  • URMC-099 [orb1226729]

    >98% (HPLC)

    1229582-33-5

    421.5368

    C27H27N5

    10 mg, 5 mg, 50 mg, 100 mg, 25 mg, 1 g, 500 mg, 200 mg
Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

URMC-099 (orb1301112)

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5 mg
¥ 2,340.00
25 mg
¥ 4,420.00
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