1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. ML216

ML216 (Synonyms: CID-49852229)

Cat. No.: HY-12342 Purity: 99.77%
Handling Instructions

ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLMfull-length and BLM636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 µM. Antitumor avtivity.

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

ML216 Chemical Structure

ML216 Chemical Structure

CAS No. : 1430213-30-1

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10 mM * 1 mL in DMSO USD 73 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLMfull-length and BLM636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 µM. Antitumor avtivity[1][2].

IC50 & Target

IC50: 2.98 μM (BLMfull-length) and 0.97 μM (BLM636-1298)[1]

In Vitro

ML216 (12.5-50 µM; 24-72 hours; PSNG5 and PSNG13cells) treatment inhibits the proliferation of PSNF5 cells in a concentration-dependent manner, but not of PSNG13 cells[1].
ML216 treatment leads to a statistically significant increase in the frequency of sister chromatid exchanges (SCEs) in PSNF5 cells, but not in PSNG13 cells[1].
ML216 increases the sensitivity of PSNF5 cells to aphidicolin but has no sensitizing effect on isogenic PSNG13 cells devoid of BLM[1].
ML216 inhibits both the full length WRN (IC50 of 5 μM) and a truncated WRN500-946 (IC50 of 12.6 μM), with the former being 2.5-fold more sensitive to inhibition. BLM is a little more sensitive than WRN to inhibition by ML216 (1.7-fold based on IC50 values). Despite the detectable inhibition of WRN by ML216, this compound appears selective for BLM in human cells. ML216 inhibits proliferation of WRN+ and WRN cells equally well, and similarly sensitized both cell types to aphidicolin[1].

Cell Proliferation Assay[1]

Cell Line: PSNG5 and PSNG13cells
Concentration: 12.5 μM or 50 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Inhibited the proliferation of PSNF5 cells, but not of PSNG13 cells, and did so in a concentration-dependent manner.
In Vivo

Although ML216 inhibits unwinding by the sequence-related BLM and WRN helicases similarly in vitro, the apparent dependence on BLM for ML216 to exert its biological effects in human cells suggests BLM specificity for the drug’s mechanism of action in vivo. A co-crystal structure of BLM in complex with inhibitor would be informative. Cellular cues in vivo may induce a specific conformation of WRN that makes it resistant to ML216[2].

Molecular Weight

383.32

Formula

C₁₅H₉F₄N₅OS

CAS No.

1430213-30-1

SMILES

O=C(NC1=CC=C(F)C(C(F)(F)F)=C1)NC2=NN=C(S2)C3=CC=NC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (52.18 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6088 mL 13.0439 mL 26.0879 mL
5 mM 0.5218 mL 2.6088 mL 5.2176 mL
10 mM 0.2609 mL 1.3044 mL 2.6088 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 99.77%

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Keywords:

ML216CID-49852229ML 216ML-216CID49852229CID 49852229DNA/RNA SynthesisAnticancerBLMDNAunwindinghelicasetoxicityanti-proliferativesisterchromatidWRNInhibitorinhibitorinhibit

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