2. TZ1104

TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia.



(Pink: CDK7 ligand (HY-183071); Blue: VHL ligand (HY-112078); Black: linker (HY-W108876)).

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TZ1104

TZ1104 화학구조

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TZ1104 Related Antibodies

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제품 설명

TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia[1].


(Pink: CDK7 ligand (HY-183071); Blue: VHL ligand (HY-112078); Black: linker (HY-W108876)).

In Vitro

TZ1104 (0.1-nM μM; 6 h) emerges as a potent CDK7 degrader and achieves a half degradation concentration (DC50) of 4.92 nM and a maximum degradation (Dmax) of 98.87% in MV4-11 cells[1].
TZ1104 (72 h) shows potent and broad CDK7 degradation across various
acute leukemia cell lines, encompassing AML (Molm13, THP-1, HL60,
CESS) and ALL (RS4;11) models[1].
TZ1104 demonstrates significantly enhanced antiproliferative effects while maintaining minimal cytotoxicity in human peripheral blood mononuclear cells (PBMCs)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TZ1104 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1 nM; 1 nM; 10 nM
Incubation Time: 6 h
Result: Emerged as a potent CDK7 degrader and achieved a half degradation concentration (DC50) of 4.92 nM and a maximum degradation (Dmax).
In Vivo

TZ1104 (50 mg/kg; i.p.; twice daily; 26 days) delivers tumor-selective CDK7 degradation and suppresses MV4-11 xenograft tumor growth in Nu/Nu mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 MV4-11 cells for a MV4-11 subcutaneous xenograft model)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily; 26 days
Result: Reduced tumor weight relative to vehicle control.
Induced robust CDK7 degradation in tumor tissues.
Caused no significant CDK7 reduction in PBMCs.
Caused no observable body weight loss during treatment.
분자량

992.69

화학식

C49H66ClN9O7S2
SMILES

O=C(N[C@H]1CC[C@H](NC2=NC=C(Cl)C(NC3=CC=CC=C3S(=O)(C(C)C)=O)=N2)CC1)CCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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TZ1104 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TZ1104TZ 1104TZ-1104proteasomeRNA polymerase II CTD Ser5cyclin HCDK2 Thr160VHL E3 ligaseCDK1 Thr161CDK7xenograft modelsMAT1acute leukemia cellsInhibitorinhibitorinhibit

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TZ1104
Cat. No.:
HY-183073
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