MedKoo Cat#: 555506 | Name: HG-10-102-01
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 20.3 nM). HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant. HG-10-102-01 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 µM in cells and is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.

Chemical Structure

HG-10-102-01
HG-10-102-01
CAS#1351758-81-0

Theoretical Analysis

MedKoo Cat#: 555506

Name: HG-10-102-01

CAS#: 1351758-81-0

Chemical Formula: C17H20ClN5O3

Exact Mass: 377.1255

Molecular Weight: 377.83

Elemental Analysis: C, 54.04; H, 5.34; Cl, 9.38; N, 18.54; O, 12.70

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,850.00 2 Weeks
2g USD 4,950.00 2 Weeks
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Synonym
HG-10-102-01; HG 10-102-01; HG10-102-01; HG-1010201; HG 1010201; HG1010201;
IUPAC/Chemical Name
[4-[[5-chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinyl-methanone
InChi Key
YEVOZZZLKJKCCD-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)
SMILES Code
O=C(C1=CC=C(NC2=NC=C(Cl)C(NC)=N2)C(OC)=C1)N3CCOCC3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target
Product Data
Biological target:
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.
In vitro activity:
Compound 4 (HG-10-102-01) induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells (Figure 3a). Reference: ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. https://pubmed.ncbi.nlm.nih.gov/23066449/
In vivo activity:
4 (HG-10-102-01) induced similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells and mouse embryonic fibroblast cells (Figure 4b,c). Reference: ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. https://pubmed.ncbi.nlm.nih.gov/23066449/
Solvent mg/mL mM
Solubility
DMF 10.0 26.47
DMSO 40.0 105.87
DMSO:PBS (pH 7.2) (1:4) 0.2 0.53
Ethanol 0.3 0.79
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 377.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. doi: 10.1021/ml300123a. Epub 2012 Jun 18. PMID: 23066449; PMCID: PMC3467149.
In vitro protocol:
1. Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. doi: 10.1021/ml300123a. Epub 2012 Jun 18. PMID: 23066449; PMCID: PMC3467149.
In vivo protocol:
1. Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. doi: 10.1021/ml300123a. Epub 2012 Jun 18. PMID: 23066449; PMCID: PMC3467149.