bcr-abl

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, induces Bcr-Abl degradation via the ubiquitin-proteasome pathway and exhibits antiproliferative effects on K562 cells, indicating its potential in cancer research [1].

SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours.

SNIPER(ABL)-013, a compound that links GNF5 (ABL inhibitor) with Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 20 μM[1].

SNIPER(ABL)-015, a compound that conjugates GNF5 (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 5 μM [1].

SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a DC50 of 0.3 μM[1].

SNIPER(ABL)-020 is a chemical compound consisting of Dasatinib, an ABL inhibitor, and Bestatin, an IAP ligand, conjugated with a linker. This compound effectively reduces the BCR-ABL protein[1].

SNIPER(ABL)-024, a compound that conjugates GNF5 (ABL inhibitor) to an LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a half-maximal degradation concentration (DC50) of 5μM[1].

SNIPER(ABL)-033, a compound that conjugates HG-7-85-01 (ABL inhibitor) to a LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a DC50 of 0.3 μM[1].

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to an LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM for ABL, 10 nM for cIAP1, 12 nM for cIAP2, and 50 nM for XIAP[1].

SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a DC50 value of 10 μM[1].

SNIPER(ABL)-047, a compound that links HG-7-85-01 (an ABL inhibitor) to MV-1 (an IAP ligand) via a linker, effectively decreases the BCR-ABL protein levels, achieving a DC50 value of 2 μM[1].

SNIPER(ABL)-049, a compound that conjugates Imatinib (ABL inhibitor) with Bestatin (IAP ligand) through a linker, effectively reduces BCR-ABL protein levels, demonstrating a DC50 of 100 μM[1].

SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1].

SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein levels, achieving a half-maximal degradation concentration (DC50) of 10 μM[1].

SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy. It is primarily utilized in the investigation of chronic myeloid leukemia (CML) [1].

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with a DC50 of 2.7 nM, used in chronic myeloid leukemia (CML) research [1].

ML 2-23 is a potent BCR-ABL degrader functioning as a PROTAC, demonstrating selective proteasome-dependent degradation of BCR-ABL in leukemia cells [1].

GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of th

SJ11646 is a Dasatinib-based LCK PROTAC degrader with a DC50 of 0.00838 pM. It exhibits potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, significantly prolongs LCK signal inhibition, and induces apoptosis in T-ALL cells. SJ11646 binds with high affinity to 51 human kinases, particularly ABL1, KIT, and DDR1. In mouse models of T-ALL, SJ11646 demonstrates exceptional anti-leukemic efficacy.

DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP ligand via a linker to form SNIPER. N-Deshydroxyethyl Dasatinib is used in the study of cancer and immune diseases.

HG-7-85-01-NH2, as the ligand for SNIPER(ABL)-033, effectively induces the reduction of BCR-ABL protein. This is achieved through SNIPER(ABL)-033, which connects HG-7-85-01 (an ABL inhibitor) to an LCL161 derivative (an IAP ligand) using a linker, demonstrating a DC50 value of 0.3 μM [1].

MRT-7612 (Compound 4) is a cereblon-based molecular glue degrader targeting tyrosine kinases. It significantly induces the degradation of HCK and LYN, with a comparatively weaker effect on LCK. MRT-7612 is applicable in research related to cancers such as chronic myeloid leukemia, autoimmune disorders, and chronic inflammatory diseases.