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UM 729 Enhancer of AhR antagonists

Catalog No.A8952
Size Price Stock Qty
10mM (in 1mL DMSO)
$160.00
In stock
5mg
$138.00
In stock
25mg
$348.00
In stock
100mg
$698.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

UM 729

Protocol

Cell experiment [1]:

Cell lines

Human AML cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 ?M; 4 days

Applications

UM 729 inhibited AML cell differentiation. In 05H163 cells, AhR suppressors (flavonoid, benzothiophene, and β-carboline) combined UM 729 increased the numbers of CD34+CD15-cells. In most AML specimens, UM 729 exhibited an additive effect with AhR antagonists in inhibiting cell differentiation.

Animal experiment [1]:

Animal models

NSG mice

Dosage form

1 ?M; i.v.

Applications

In NSG mice, UM 729 administered alone or in combination with SR1 increased AML cell engraftment but not leukemic stem cell frequency.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Pabst C1, Krosl J1, Fares I1, Boucher G1, Ruel R1, Marinier A2, Lemieux S3, Hébert J4, Sauvageau G4.Identification of small molecules that support human leukemia stem cell activity ex vivo. Nat Methods. 2014 Apr;11(4):436-42.

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Chemical Properties

Cas No. 1448723-60-1 SDF Download SDF
Chemical Name methyl 4-((3-(piperidin-1-yl)propyl)amino)-9H-pyrimido[4,5-b]indole-7-carboxylate
Canonical SMILES O=C(OC)C1=CC=C(C2=C(NCCCN3CCCCC3)N=CN=C2N4)C4=C1
Formula C20H25N5O2 M.Wt 367.44
Solubility >36.7mg/ml in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

UM729 is a small molecule enhancer of AhR antagonists [1].

UM729 has been found to be a new pyrimidoindole and have an additive efficacy with AhR antagonists in preventing differentiation in most AML specimen. In addition, UM729 has been reported to expand mormal HSPCs in a AhR-independent fashion. Moreover, UM729 has shown an additive effect with AhR inhibitors(SR1) on the ex vivo culture of primary human AML cells(05H163 cells) and progenitor cells [1]. Besides, UM729 has been revealed to expand HSCs and synergize with SR1 to enhance human HSC expansion, result in successful long-term engraftment of SCID repopulating cells (SRCs) in immunodeficient mice [2].

References:
[1] Pabst C1, Krosl J1, Fares I1, Boucher G1, Ruel R1, Marinier A2, Lemieux S3, Hébert J4, Sauvageau G4.Identification of small molecules that support human leukemia stem cell activity ex vivo. Nat Methods. 2014 Apr;11(4):436-42.
[2] Watts K L, Chandrasekaran D, Sauvageau G, et al. Effective Expansion and Engraftment Of Nonhuman Primate CD34+ Hematopoietic Stem Cells After Co-Culture With The Small Molecule UM171[J]. Blood, 2013, 122(21): 1656-1656.