THZ1 2HCl - Moligand™, 10mM in DMSO , Inhibitor of cyclin dependent kinase 7, CAS No.1604810-83-4(freebase), Inhibitor of cyclin dependent kinase 7

CAS: 1604810-83-4(freebase) Cat. No.: T408846 Summenformel: C₃₁H₃₀Cl₃N₇O₂ Molekulargewicht: 638.97

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-​[3-​[[5-​chloro-​4-​(1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-​4-​[[(2E)​-​4-​(dimethylamino)​-​1-​oxo-​2-​buten-​1-​yl]​amino]​-Benzamide dihydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

THZ1 is a covalentCDK7inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
In vitro

THZ1 uses a unique mechanism, combining ATP-site and allosteric covalent binding, as a means of attaining potency and selectivity for CDK7. THZ1 irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7. THZ1, but not THZ1-R, completely inhibits the phosphorylation of the established intracellular CDK7 substrate RNAPII CTD at Ser\u20095 and Ser\u20097, with concurrent loss of Ser\u20092 phosphorylation at 250\u2009nM in Jurkat cells. THZ1 exhibits strong antiproliferative effects across a broad range of cancer cell lines from various cancer types. In Jurkat cells, low-dose THZ1 has a profound effect on a small subset of genes, including the key regulator RUNX1, thus contributing to subsequent loss of the greater gene expression program and cell death. THZ1 causes defects in Pol II(polymerase II) phosphorylation, co-transcriptional capping, promoter proximal pausing, and productive elongation.

In vivo

THZ1 reduces the proliferation of KOPTK1 T-ALL cells in a human xenograft mouse model. THZ1 is well tolerated at 10 mg/kg with no observable body weight loss or behavioural changes, suggesting that it causes no overt toxicity in the animals.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：4 h

Powder Purity:≥97%

Specifications

Synonyme

N-​[3-​[[5-​chloro-​4-​(1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-​4-​[[(2E)​-​4-​(dimethylamino)​-​1-​oxo-​2-​buten-​1-​yl]​amino]​-Benzamide dihydrochloride

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of cyclin dependent kinase 7

Namen und Kennungen

• Molekulargewicht: 638.97

Zugehörige Ziele (menschlich)

CDK7 Tchem Cyclin-dependent kinase 7 (1 Activities)

Discover Target: CDK7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 63 mg/mL warmed with 50ºC Water: bath (199.74 mM); Water: Insoluble; Ethanol: Insoluble

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1604810-83-4(freebase), the molecular formula is C31H30Cl3N7O2, and the molecular weight is 638.97 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.