NF-κB

Cat. No.

A24835

CAS No.

2655656-99-6

Zomiradomide

Synonyms: KT-413

Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses.

Cat. No.

A25074

CAS No.

2782022-40-4

LD4172

LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research.

Cat. No.

A25449

CAS No.

3037417-26-5

TD1092

TD1092 is a PROTAC that functions as a pan-IAP degrader, effectively targeting cIAP1, cIAP2, and XIAP. By promoting the degradation of IAPs, TD1092 activates Caspase 3/7, leading to apoptosis in cancer cells. Additionally, it inhibits the TNFα-mediated NF-κB signaling pathway, reducing the phosphorylation of IKK, IkBα, p65, and p38. This compound is primarily used in cancer research to explore mechanisms of apoptosis and therapeutic resistance.

Cat. No.

A26045

CAS No.

2417369-99-2

GNE-5472

GNE-5472 is a potent bifunctional degrader targeting estrogen receptor alpha (ERα) through the PRRTAC mechanism. By functioning as a pan-IAP antagonist, GNE-5472 inhibits cIAP1/2, thereby activating the non-classical NF-κB pathway, which leads to significant upregulation of TNFα expression. This compound effectively inhibits the proliferation of breast cancer cells and promotes apoptosis. GNE-5472 is valuable for research applications in the study of breast cancer and related signaling pathways.

Cat. No.

A26156

CAS No.

3091132-73-6

FIP22

FIP22 is a potent and selective degrader of IRAK4 utilizing the PROTAC technology. It functions by inducing degradation through the formation of a ternary complex consisting of IRAK4, FIP22, and CRBN, with an EC50 of 12.63 nM. This mechanism effectively inhibits IRAK4-mediated signaling pathways, including NF-κB and MAPK pathways, making FIP22 valuable for research into conditions such as atopic dermatitis, where IRAK4 plays a critical role.

Cat. No.

A26221

CAS No.

3070346-91-4

R1-ICR-5

R1-ICR-5 is a selective RIPK1 PROTAC degrader designed to mediate protein degradation via the VHL pathway. This compound promotes the degradation of RIPK1, subsequently dysregulating TNFR1 and TLR3/4 signaling pathways, enhancing the activity of NF-κB, MAPK, and IFN signaling. Additionally, R1-ICR-5 facilitates RIPK3 activation, leading to necroptosis. This reagent is applicable in research focused on triple-negative breast cancer and skin inflammation.

Cat. No.

A26537

CAS No.

2978763-95-8

HD-TAC7

HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD).

Cat. No.

A30885

CAS No.

3105680-00-7

PROTAC XPO1 degrader-1

PROTAC XPO1 degrader-1 is a targeted protein degrader designed to selectively promote the degradation of XPO1. This compound demonstrates significant anti-proliferative effects, induces apoptosis, inhibits NF-κB signaling, and causes cell cycle arrest at the G1 phase. It is an important tool for researching hematological malignancies, offering insights into therapeutic strategies by modulating XPO1 levels.

Cat. No.

A34408

CAS No.

2767204-39-5

PROTAC BTK Degrader-6

PROTAC BTK Degrader-6 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 of 3.18 nM. This compound exhibits anti-inflammatory activity by inhibiting NF-κB activation and reducing the expression of pro-inflammatory cytokines, including IL-1β and IL-6. It serves as a valuable tool for research into the modulation of immune responses and the development of therapies for inflammatory diseases.

Cat. No.

A36893

CAS No.

3032576-92-1

INNO-220

INNO-220 is a CRBN-dependent molecular glue degrader that specifically targets CK1α. This orally active compound induces cell cycle arrest at the G0/G1 phase and promotes apoptosis through the degradation of CK1α. Additionally, INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, effectively inhibiting NF-κB signaling in stimulated T cells and lymphoma cells with activating mutations in CARD11. This reagent serves as a valuable tool for advancing research in lymphoma.

Cat. No.

A42445

CAS No.

793719-01-4

EN450

EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. By engaging with allosteric C111 in the E2 ubiquitin ligase UBE2D, EN450 facilitates the formation of a ternary complex involving UBE2D and NFKB1. This interaction leads to the degradation of NF-κB, resulting in notable anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism. EN450 serves as a valuable tool for research involving NF-κB signaling and its implications in cancer biology.

Cat. No.

A65574

CAS No.

3109967-69-0

PROTAC STING degrader-3

PROTAC STING degrader-3 is a potent STING PROTAC degrader that operates through the ubiquitin-proteasome pathway, exhibiting a DC50 of 0.62 μM. This compound facilitates STING degradation, resulting in the inhibition of STING/TBK1/NF-κB signaling, thereby exerting notable anti-inflammatory effects. Additionally, PROTAC STING degrader-3 demonstrates renal protective properties and serves as a valuable tool for investigating acute kidney injury (AKI).

Cat. No.

A76597

CAS No.

2086298-33-9

(S,R,S)-AHPC-Boc derivative 1

Synonyms: VH032-Boc derivative 1

(S,R,S)-AHPC-Boc derivative 1 is a selective proteasomal degrader that targets MALT1. By recruiting the E3 ubiquitin ligase CRBN, it forms a ternary complex with MALT1, facilitating its ubiquitination and subsequent proteasomal degradation. This compound inhibits the NF-κB signaling pathway by disrupting the CBM complex, which may induce apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is valuable for the investigation of MALT1-dependent cancers, particularly diffuse large B-cell lymphoma (DLBCL).

Cat. No.

A79551

CAS No.

2756388-01-7

BSJ-05-037

BSJ-05-037 is an ITK PROTACs degrader that efficiently induces the degradation of ITK in T-cell lymphoma cell lines. This compound inhibits the NF-κB/GATA-3 signaling pathway and decreases PLCγ1 phosphorylation, thereby reducing the proliferation of T-cell lymphoma cells. Additionally, BSJ-05-037 enhances the sensitivity of these cancer cells to chemotherapy. In mouse models, it has shown the ability to diminish GATA-3 expression, lower tumor volume, and counteract chemotherapy resistance, making it a valuable tool for research on T-cell lymphoma.

Cat. No.

A79587

CAS No.

3100147-70-1

JP-163-16

JP-163-16 is a RelA/p65 PROTAC degrader that facilitates the selective degradation of RelA/p65 via the proteasome pathway. By inhibiting the NF-κB signaling pathway, JP-163-16 promotes apoptosis in cells, making it a valuable tool for investigating RelA/p65-dependent tumors, including chronic lymphocytic leukemia (CLL). This compound is instrumental for studies aimed at understanding the role of NF-κB in cancer progression and therapeutic resistance.

Cat. No.

B22084

CAS No.

3104855-98-0

PSP-0119

PSP-0119 is a highly selective PROTAC degrader targeting IRAK4, demonstrating an IC50 of 2.83 nM. This compound effectively inhibits IRAK4 kinase activity, NF-κB signaling, and IL-1β-induced IRAK4 phosphorylation. Notably, PSP-0119 induces degradation of IRAK4 specifically in FLT3-mutant acute myeloid leukemia (AML) cell lines while sparing FLT3-wild-type AML cells and normal bone marrow. It serves as a valuable tool for research into the mechanisms underlying AML, particularly in targeting aberrant IRAK4 activity.