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Harmine hydrochloride ADC Cytotoxin chemical

Name: Harmine hydrochloride
Brand: Selleck Chemicals
SKU: S3817
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S3817

Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.

Chemical Structure

Molecular Weight: 248.71

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77
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Chemical Information, Storage & Stability

Molecular Weight	248.71	Formula	C₁₃H₁₂N₂O.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	343-27-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Telepathine hydrochloride			Smiles	CC1=NC=CC2=C1NC3=C2C=CC(=C3)OC.Cl

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.100mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DYRK1A ^[1] (Cell-free assay) 33 nM MNB ^[1] (Cell-free assay) 149 nM DYRK1B ^[1] (Cell-free assay) 166 nM DYRK2 ^[1] (Cell-free assay) 1.9 μM
In vitro	Harmine inhibits substrate phosphorylation by DYRK1A more potently than it inhibits substrate phosphorylation by the closely related kinase DYRK1B [half maximal inhibitory concentrations (IC50) of 33 nM versus 166 nM, respectively] and by the more distant members of the family, DYRK2 and DYRK4 (1.9 μM and 80 μM, respectively). Much higher concentrations of harmine are required to suppress tyrosine autophosphorylation of the translational intermediate of DYRK1A in a bacterial in vitro translation system (IC50 = 1.9 μM). Harmine inhibits the phosphorylation of a specific substrate by DYRK1A in cultured cells with a potency similar to that observed in vitro (IC50=48 nM), without negative effects on the viability of the cells. Harmine does not inhibit tyrosine autophosphorylation of DYRK1A in HEK293 cells^[1]. Harmine is able to induce beta cell proliferation, increase islet mass and improve glycemic control. It is a CNS stimulant^[2].
In vivo	In a partial pancreatectomy (PPX) model, harmine treatment induces Ki-67 labeling in beta cells in both sham-operated mice and in mice subjected to PPX, with the most robust proliferation in the beta cells of harmine-treated PPX mice. In the PPX model, regeneration of beta cell mass is substantially more rapid in the harmine-treated mice than in the controls, reaching near-normal values in only 14 d. In a euglycemic nonobese diabetic-severe combined immunodeficiency (NOD-SCID) mouse model, BrdU and Ki-67 labeling is two- to threefold higher in human beta cells transplanted into the renal capsule of harmine-treated compared to control euglycemic mice, without evidence of beta cell death. In a marginal mass human islet transplant model in streptozotocin-diabetic NOD-SCID mice, harmine treatment also results in near normal glycemic control. Harmine induces production of the important beta cell transcription factors NKX6.1, PDX1 and MAFA.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19796173/ [2] https://pubmed.ncbi.nlm.nih.gov/25751815/ [3] https://pubmed.ncbi.nlm.nih.gov/17488638/

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