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Home > Molecular Glues

HQ461

  Cat. No.:  DC60254   Featured
Chemical Structure
1226443-41-9
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More than 5000 active chemicals with high quality for research!
Field of application
HQ461 is a molecular glue degrader that facilitates the interaction between CDK12 and the DDB1-CUL4-RBX1 E3 ubiquitin ligase, resulting in the polyubiquitination and subsequent degradation of the CDK12-interacting protein Cyclin K (CCNK). This degradation impairs CDK12 function, leading to reduced phosphorylation of its substrates, downregulation of DNA damage response genes, and ultimately, cell death.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1226443-41-9
Chemical Name: 2-[2-[(6-Methylpyridin-2-yl)amino]-1,3-thiazol-4-yl]-N-(5-methyl-1,3-thiazol-2-yl)acetamide
Synonyms: VU0528787-1;2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide;2-[2-[(6-Methylpyridin-2-yl)amino]-1,3-thiazol-4-yl]-N-(5-methyl-1,3-thiazol-2-yl)acetamide
SMILES: S1C([H])=C(C([H])([H])C(N([H])C2=NC([H])=C(C([H])([H])[H])S2)=O)N=C1N([H])C1=C([H])C([H])=C([H])C(C([H])([H])[H])=N1
Formula: C15H15N5Os2
M.Wt: 345.4425
Purity: 98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC60864 D927 (DS11252927) D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
DC60863 D223 (DS02312223) D223 is a molecular glue and promotes glucose uptake in the absence of insulin. D223 also increases the affinity of RAS binding to PI3Kα by ~500-fold.
DC60858 LC-04-045 LC-04-045 is a leading NEK7 molecular glue degrader with DC50 of 7 nM and Dmax of 90 % in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome.
DC60852 PVTX-405 PVTX-405 is a potent, effective, highly selective, and orally efficacious IKZF2 molecular glue degrader with DC50 of  0.7 nM. PVTX-405 in combination with anti-PD1 or anti-LAG3 significantly increases animal survival compared to anti-PD1 or anti-LAG3 alone.
DC60837 MGD-28 MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.
DC67413 MRT-23227
DC67412 MRT-3486 MRT-3486 (Compound 5) is a cereblon-based NEK7 molecular glue degrader. MRT-3486 can be used for autoinflammatory diseases research.
DC67411 MRT-7612
DC67410 MRT-10350
DC67407 IKZF1-degrader-1 IKZF1-degrader-1 (Compound 9-B) is a highly potent molecular glue that achieves sub-nanomolar degradation of IKZF1 (DC50 = 0.134 nM), demonstrating significant therapeutic potential for targeting IKZF1-dependent malignancies.
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