THZ 531
CAS No. 1702809-17-3
THZ 531 ( THZ531 )
Catalog No. M12601 CAS No. 1702809-17-3
THZ 531 (THZ531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
2MG | 75 | In Stock |
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5MG | 102 | In Stock |
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10MG | 140 | In Stock |
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25MG | 312 | In Stock |
|
50MG | 447 | In Stock |
|
100MG | 651 | In Stock |
|
500MG | 1341 | In Stock |
|
1G | Get Quote | In Stock |
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Biological Information
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Product NameTHZ 531
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NoteResearch use only, not for human use.
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Brief DescriptionTHZ 531 (THZ531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively.
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DescriptionTHZ 531 (THZ531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively; dispalys 50-fold selectivity over CDK7 and CDK9 (IC50 of 8.5 and 10.5 uM, respectively), and shows no appreciable inhibitory effect on ERK1; irreversiblely inhibits Jurkat cell proliferation with an IC50 of 50 nM, induces apoptosis in a dose- and time-dependent manner with low doses (<350 nM); selectively reduced Ser2 phosphorylation levels without appreciable effect on CTD pSer5/pSer7 levels, causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II, inhibits DDR and transcription factor gene expression.
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SynonymsTHZ531
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PathwayAngiogenesis
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TargetCDK
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RecptorCDK12,CDK13
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Research AreaOther Indications
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Indication——
Chemical Information
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CAS Number1702809-17-3
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Formula Weight558.08
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Molecular FormulaC30H32ClN7O2
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Purity>98% (HPLC)
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SolubilityDMSO: Soluble ( < 1 mg/ml refers to the product slightly soluble or insoluble )
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SMILESO=C(NC1=CC=C(C(N2C[C@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2)=O)C=C1)/C=C/CN(C)C
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Chemical Name(R,E)-N-(4-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Zhang T, et al. Nat Chem Biol. 2016 Oct;12(10):876-84.
2. Paculová H, et al. Cell Div. 2017 Oct 27;12:7. doi: 10.1186/s13008-017-0033-x.
3. Iniguez AB, et al. Cancer Cell. 2018 Jan 17. pii: S1535-6108(17)30561-5.
2. Paculová H, et al. Cell Div. 2017 Oct 27;12:7. doi: 10.1186/s13008-017-0033-x.
3. Iniguez AB, et al. Cancer Cell. 2018 Jan 17. pii: S1535-6108(17)30561-5.
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