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(rel)-MC180295 (Synonyms: (rel)-MC180295)

Catalog No.GC34124

(rel)-MC180295 ((rel)-(rel)-MC180295) es un inhibidor potente y selectivo de CDK9-Cyclin T1, con una IC50 de 5 nM, al menos 22 veces mÁs selectivo para CDK9 que para otras CDK. (rel)-MC180295 también inhibe GSK-3α y GSK-3β. (rel)-MC180295 ((rel)-(rel)-MC180295) tiene un potente efecto antitumoral.

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(rel)-MC180295 Chemical Structure

Cas No.: 2237942-08-2

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
218,00 $
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5mg
198,00 $
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10mg
320,00 $
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50mg
1.053,00 $
Disponible
100mg
1.477,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of (rel)-MC180295

(rel)-MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. (rel)-MC180295 also inhibits GSK-3α and GSK-3β. (rel)-MC180295 has potent anti-tumor effect[1].

(rel)-MC180295 (MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). (rel)-MC180295 also inhibits GSK-3α and GSK-3β[1].(rel)-MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].(rel)-MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1].

(rel)-MC180295 (MC180295; 20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1].

[1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.

Chemical Properties of (rel)-MC180295

Cas No. 2237942-08-2 SDF
Sinónimos (rel)-MC180295
Canonical SMILES NC1=C(C(C2=CC=CC=C2[N+]([O-])=O)=O)SC(N[C@@H]3[C@H](C4)CC[C@H]4C3)=N1
Formula C17H18N4O3S M.Wt 358.41
Solubility DMSO : 100 mg/mL (279.01 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (rel)-MC180295

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1 mg 5 mg 10 mg
1 mM 2.7901 mL 13.9505 mL 27.901 mL
5 mM 0.558 mL 2.7901 mL 5.5802 mL
10 mM 0.279 mL 1.3951 mL 2.7901 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 35 reference(s) in Google Scholar.)

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