BSJ-05-037|degrader of ITK|DC Chemicals

Cas No.:	2756388-01-7
Chemical Name:	Autotaxin-IN-8
SMILES:	COC1=CC(C)=C(SC2=CN=C(NC(=O)C3=CC=C(N4CCN(CCCCCCCNC(=O)COC5=C6C(=O)N(C7CCC(=O)NC7=O)C(=O)C6=CC=C5)CC4)C=C3)S2)C=C1C(=O)N1CCN(C(C)=O)CC1
Formula:	C₅₁H₅₉N₉O₁₀S₂
M.Wt:	1022.2
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	Jiang B, et al. Cell Chem Biol. 2023 Mar 27:S2451-9456(23)00086-7.

Cat. No.	Product name	Field of application
DC67177	BTK-IN-29	BTK-IN-29 (compound 14) is an inhibitor of Btk.
DC65810	KT-333	KT-333 is a first-in-class molecular glue that induces selective degradation of STAT3 via the ubiquitin-proteasome system by simultaneously engaging STAT3 and the VHL E3 ligase. This novel mechanism enables potent STAT3 depletion with minimal off-target effects, demonstrating strong anti-tumor activity in hematologic malignancies.
DC55003	XY028-140 (MS140)	XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).
DC74522	WDR5 PROTAC MS40	MS40 is a cereblon (CRBN)-based proteolysis targeting chimera (PROTAC) degrader of the onco-target WD repeat domain 5 (WDR5) [1]. WDR5 is an integral component of the MLL/KMT2A lysine methyltransferase protein complex. The WDR5-binding component of MS40 is the selective inhibitor OICR-9429, and the CRBN-targeting moiety is the immunomodulatory drug pomalidomide. MS40 promotes degradation of WDR5 and the pomalidomide transcription factor neo-substrates IKZF1 and IKZF3.
DC74479	Autotaxin-IN-8	BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78. BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the proteasome. BSJ-05-037 induces GATA-3 loss and decreases chemotherapy resistance in vitro. BSJ-05-037 disrupts TCR signaling, downregulates the Th2-associated transcription factor GATA-3, and can overcome chemotherapy resistance in TCL models in vivo.
DC12022	dBET6	dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.
DC12380	BSJ-03-123	BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.

Autotaxin-IN-8