1. Autophagy
  2. LRRK2

HG-10-102-01 (Synonyms: LRRK2 inhibitor 1)

Cat. No.: HY-13488 Purity: 99.54%
Handling Instructions

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2.

For research use only. We do not sell to patients.

HG-10-102-01 Chemical Structure

HG-10-102-01 Chemical Structure

CAS No. : 1351758-81-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 147 In-stock
Estimated Time of Arrival: December 31
5 mg USD 134 In-stock
Estimated Time of Arrival: December 31
10 mg USD 186 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Description

HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2. HG-10-102-01 exhibited biochemical IC50s of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. At a concentration of 10 μM, HG-10-102-01 only inhibited the kinase activities of MLK1 and MNK2 to greater than 80% of the DMSO control. Dose-response analysis revealed inhibition of MLK1 with an IC50 2.1 μM and MNK2 with an IC50 0.6 μM. KinomeScan analysis against a near comprehensive panel of 451 kinases at a concentration of 1 μM resulted in no interactions detected with kinases other than G2019S LRRK2 with the exception of one mutant form of c-Kit (L576P) demonstrating the outstanding selectivity of this inhibitor. HG-10-102-01 significantly inhibited phosphorylation of wildtype LRRK2 and LRRK2[G2019S] mutant at Ser910 and Ser935 at 0.3-1.0 μM in cell culture, which is approximately the same potency as LRRK2-IN-1 (1). HG-10-102-01 is relatively insensitive to the A2016T mutation which suggests that this mutant will not be useful to validate whether the pharmacological effects of the compound are LRRK2-dependent. HG-10-102-01 can inhibit phosphorylation of Ser910 and Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 50 mg/kg. Further optimization of this chemo-type especially in regards to in vivo half-life will be reported in due course [1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (132.33 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6467 mL 13.2335 mL 26.4669 mL
5 mM 0.5293 mL 2.6467 mL 5.2934 mL
10 mM 0.2647 mL 1.3233 mL 2.6467 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

377.83

Formula

C₁₇H₂₀ClN₅O₃

CAS No.

1351758-81-0

SMILES

COC1=CC(C(N2CCOCC2)=O)=CC=C1NC3=NC(NC)=C(Cl)C=N3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
HG-10-102-01
Cat. No.:
HY-13488
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HG-10-102-01

Cat. No.: HY-13488