PROTAC Proteolysis Targeting Chimeric Molecules

Cat.No.	Name	Information
M40697	NX-5948	NX-5948 (BTK-IN-24) is an orally active, blood-brain barrier-penetrating, BTK-targeting degradation agent for the study of B-cell malignancies and autoimmune diseases. NX-5948 induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation.
M10423	DT2216	DT2216 is a BCL-XL protein hydrolysis targeting chimera (PROTAC) that ligates and degrades BCL-XL with E3 ubiquitin (E3) ligase. DT2216 is effective against a variety of BCL-XL-dependent leukemias and cancer cells.
M9396	A1874	A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells).
M9238	dBET6	dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
M8477	Indisulam	Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.
M7709	CR8	CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9).
M58644	Setidegrasib	Setidegrasib is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect.
M58638	PROTAC HK2 Degrader-1	PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death.
M58635	ZXH-4-130 TFA	ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC).
M58581	MS4322	MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5.
M58163	(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine	(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level.
M57286	MTX-23	MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis.
M57182	YD23	YD23 is a SMARCA2 PROTAC.
M57181	CMP98	CMP98, a PROTAC, is unable to induce degradation of VHL.
M57180	MS8815	MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader.
M57179	TD-802	TD-802 is an androgen receptor (AR) PROTAC degrader with good microsomal stability.
M57178	ARD-266	ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader.
M57177	GNE-987	GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4.
M57175	PhosTAC7	Similar to PROTACs in their ability to induce ternary complexes, PhosTAC7 focuses on recruiting a Ser/Thr phosphatase to a phosphosubstrate to mediate its dephosphorylation.
M57174	SJ995973	SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
M57173	ARD-2585	ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
M57172	XF067-68	XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5).

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PROTAC Proteolysis Targeting Chimeric Molecules

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