2412055-93-5
2412055-93-5
Chemical Structure
CG428
- CAS No.: 2412055-93-5
- Formula:C43H43FN10O6
- Molecular Weight:814.86
IUPAC Name: 2-(2,6-dioxopiperidin-3-yl)-4-((2-(3-(4-(6-(6-((R)-2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)pyridin-2-yl)piperazin-1-yl)-3-oxopropoxy)ethyl)amino)isoindoline-1,3-dione
InChIKey: FWANKJAOTQAHHR-KWRHIPAJSA-N
SMILES: O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCC(N4CCN(C5=NC(C6=CN=C7C=CC(N8[C@@H](C9=CC=CC(F)=C9)CCC8)=NN76)=CC=C5)CC4)=O)=O
Biological Activity: CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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CG428 | 98.18% | CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma. | ||||||||||||||||||||
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GNF-8625 | GNF-8625 is a broad-spectrum TRK inhibitor that can combine with Thalidomide to form a PROTAC degrader. The IC50 of GNF-8625 for inhibiting TRKA, TRKB, and TRKC are 0.8 nM, 22 nM, and 5.4 nM, respectively. | |||||||||||||||||||||
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GNF-8625 monopyridin-N-piperazine hydrochloride | 99.74% | GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1. | ||||||||||||||||||||
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Pomalidomide-C5-Dovitinib | Pomalidomide-C5-Dovitinib is a heterobifunctional PROTAC that recruits KEAP1 E3 ligase to degrade BRD4 and BRD3, but not BRD2. | |||||||||||||||||||||
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DDC-01-163 | 99.05% | DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer. | ||||||||||||||||||||
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MS177 | 99.55% | MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest. | ||||||||||||||||||||
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NU223612 | 99.41% | NU223612 is a cereblon (CRBN)-recruiting IDO1 PROTAC degrader, with a DC50 value of 0.329-0.5438 μM against human IDO1, and it is capable of penetrating the blood-brain barrier. NU223612 directly binds to IDO1, mediates the degradation of both wild-type and catalytically inactive mutant IDO1 proteins, and does not degrade TDO2. NU223612 inhibits IDO1-mediated enzymatic activity. NU223612 directly binds to CRBN and promotes the formation of a cooperative ternary complex with IDO1. NU223612 induces ubiquitin-dependent proteasomal degradation of the IDO1 protein. NU223612 suppresses IDO1-mediated non-enzymatic phosphorylation of NF-κB p65 and the DNA-binding activity of downstream transcription factors. NU223612 can be used in studies of glioblastoma (malignant glioma). | ||||||||||||||||||||
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YD23 | 98.80% | YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC). | ||||||||||||||||||||
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JH-XII-03-02 | 99.33% | JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. JH-XII-03-02 promotes ubiquitination and degradation of LRRK2. JH-XII-03-02 can be used for the research of Parkinson's disease. | ||||||||||||||||||||
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CG428-NEG | 97.6% | CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with Kd values of 0.88 nM, 4.8 nM and 59.8 nM, respectively. CG428-NEG inhibits the growth of cancer cells and reduces the level of TPM3-TRKA fusion protein in cancer cells. CG428-NEG can be used in the research of colorectal cancer. | ||||||||||||||||||||
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PROTAC HPK1 Degrader-1 | 99.70% | PROTAC HPK1 Degrader-1 (compound B1) is a PROTAC degrader that recruits cereblon to induce HPK1 degradation, with a DC50 of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits HPK1 kinase activity, with an IC50 of 140.5 nM. PROTAC HPK1 Degrader-1 suppresses the phosphorylation of SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 can be used to investigate non-kinase-dependent signaling of HPK1 in the TCR pathway and cancer-related research. | ||||||||||||||||||||
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