1702809-17-3
1702809-17-3
Chemical Structure
THZ531
- CAS No.: 1702809-17-3
- Formula:C30H32ClN7O2
- Molecular Weight:558.07
IUPAC 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
InChIKey: RUBYHLPRZRMTJO-MOVYNIQHSA-N
SMILES: ClC(C(C1=CNC2=CC=CC=C12)=N3)=CN=C3N[C@@H]4CCCN(C(C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5)=O)C4
Biological Activity: THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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THZ531 | 99.23% | THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively. | ||||||||||||||||||||
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THZ531 (Standard) | ≥98% | THZ531 (Standard) is the analytical standard of THZ531 (HY-103618). This product is intended for research and analytical applications. THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively. | ||||||||||||||||||||
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THZ2 | 99.03% | THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM. | ||||||||||||||||||||
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Mevociclib | 99.73% | Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors. | ||||||||||||||||||||
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THZ-P1-2 | 99.86% | THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines. | ||||||||||||||||||||
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NT-1 | 99.40% | NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFRWT with an IC50 of 0.4 nM. NT-1 also inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M. NT-1 exerts deeper inhibition on p-EGFR and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research. | ||||||||||||||||||||
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BSJ-01-175 | 99.88% | BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells. | ||||||||||||||||||||
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YL5084 | 98.13% | YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner. | ||||||||||||||||||||
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ZSQ836 | ZSQ836 is an orally active dual covalent inhibitor of CDK12/CDK13, with an EC50 value of 32 nM against CDK12. ZSQ836 can induce apoptosis and exhibit anticancer activity in vivo. ZSQ836 can be used in the study of ovarian cancer. | |||||||||||||||||||||
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THZ1-R | 98.05% | THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM. | ||||||||||||||||||||
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THZ1 | 98.43% | THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression. | ||||||||||||||||||||
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(E/Z)-THZ1 dihydrochloride | (E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect. | |||||||||||||||||||||
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