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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
RIPK1 Degraders
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "RIPK1 Degraders" in MCE Product Catalog:
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Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
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1 Cited Publications
Cat. No.: HY-171658
CAS No.: 3070346-91-4
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R1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation .
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1 Cited Publications
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ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins .
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1 Cited Publications
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PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death .
Cat. No.: HY-153598
CAS No.: 2782022-40-4
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LD4172 is a selective RIPK1 PROTAC degrader with a Ki of 4.8 nM. LD4172 induces RIPK1 protein degradation via ternary complex formation with RIPK1 and VHL E3 ligase, driving ubiquitination and proteasomal breakdown. LD4172 abrogates TNF-induced classical NF-κB signaling in TRAF2-deficient cells, impairing IκBα phosphorylation and degradation, and reducing IL-8 production. LD4172 induces apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy. LD4172 acts as a chemical probe for investigating RIPK1 scaffolding functions. LD4172 can be used for the research of melanoma, colon cancer .
Cat. No.: HY-175370
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PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 induces complete degradation of RIPK1 through the ubiquitin-proteasome system by bridging the target protein RIPK1 and VHL E3 ubiquitin ligase. PROTAC RIPK1 Degrader-1 is applicable to melanoma-related research .
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PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK)
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DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades 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. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity .
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PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK NEKs
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DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade 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. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .
Cat. No.: HY-179234
LD5097 is a highly effective and selective PROTAC degrader targeting RIPK1. LD5097 can rapidly and efficiently downregulate RIPK1 and significantly enhance TNFα-mediated apoptosis in Jurkat cells. LD5097 significantly increases the levels of cleaved caspase-3/7 and PARP. LD5097 can be used for the study of acute T-lymphoblastic leukemia .
Cat. No.: HY-175371
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RIPK1-ligand-2 is a RIPK1 inhibitor. RIPK1-ligand-2 can be used for synthesis of PROTAC RIPK1 Degrader-1 (HY-175370) .
Cat. No.: HY-175374
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RIPK1 ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for RIPK1 (HY-175371) and a PROTAC linker (HY-175373), which recruits E3 ligases. RIPK1 ligand-Linker Conjugate-1 can be used for synthesis of PROTAC RIPK1 Degrader-1 (HY-175370) .
Cat. No.: HY-175373
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Bispiperidin-piperazin-acetate is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC RIPK1 Degrader-1 (HY-175370) .
Cat. No.: HY-179236
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Pip-Py-alkynyl-Ph-COOH is a PROTAC linker that can be used for the synthesis of PROTACs, such as LD5097 (HY-179234). LD5097 is a potent RIPK1 PROTAC degrader with anti-tumor activity .
Cat. No.: HY-179235
CAS No.: 2782024-39-7
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RIPK1-IN-37 is an RIPK1 inhibitor and a ligand for the target protein for PROTAC LD5097 (HY-179234). RIPK1-IN-37 can be used to synthesize PROTAC .
Cat. No.: HY-187500
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Akt RIMTAC-1 is a Akt RIMTAC degrader (a PROTAC-like agent) with a DC50 of 3.52 μM. Akt RIMTAC-1 forms a ternary complex with AKT and RIPK1, and recruits the VHL E3 ligase complex to mediate ubiquitination and proteasomal degradation. Akt RIMTAC-1 does not alter AKT1 mRNA levels (pink: AKT ligand-5 (HY-187501); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-23166)) .
Cat. No.: HY-187391
CAS No.: 3033385-55-3
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RIPK1-ligand-4 is a RIMTAC E3 recruiting ligand that indirectly recruits VHL E3 ligases by binding to RIPK1 and hijacking the endogenous RIPK1-VHL complex. RIPK1-ligand-4 can be used to synthesize the BRD4 RIMTAC-1 (HY-187390) PROTAC degrader .
Cat. No.: HY-187502
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Jak1 RIMTAC-1 is a JAK1 RIMTAC degrader (a PROTAC-like agent) with a DC50 of 322.8 nM. Jak1 RIMTAC-1 forms a ternary complex with JAK1 and RIPK1, thereby recruiting the VHL E3 ligase complex to ubiquitinate JAK1 via the ubiquitin-proteasome system and mediate its subsequent proteasomal degradation. Jak1 RIMTAC-1 does not alter JAK1 mRNA levels (pink: Jak1 ligand-1 (HY-187503); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-B0704)) .
Cat. No.: HY-187390
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BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on the RIPK1-mediated targeted chimera (RIMTAC) technology. It hijacks the endogenous RIPK1-VHL complex via the RIPK1 inhibitor moiety to indirectly recruit the VHL E3 ligase, forming a BRD4-Compound 10-RIPK1-VHL quaternary complex, and degrades BRD4 through the ubiquitin-proteasome system (UPS). BRD4 RIMTAC-1 exhibits selectivity over other BET proteins, induces concentration- and time-dependent, reversible post-translational degradation of BRD4 without altering the target mRNA level. BRD4 RIMTAC-1 potently induces endogenous BRD4 degradation in RAW264.7 and HEK-293T cells, with DC50 values of 179.1 nM and 54.12 nM, respectively. BRD4 RIMTAC-1 can be used for the research of cancer and inflammation-related diseases .
Cat. No.: HY-116356
CAS No.: 1629730-92-2
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BRD4 ligand 17 is the target protein ligand of BRD4 RIMTAC-1 (HY-187390). BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on RIPK1-mediated targeted chimeric (RIMTAC) technology, which can be used for research on cancer and inflammation-related diseases .
Cat. No.: HY-179242
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RIPK1-IN-37-CO-Ph-alkynyl-Py-Pip is a Ligand-Linker conjunction, targeting RIPK1. RIPK1-IN-37-CO-Ph-alkynyl-Py-Pip can be used to synthesize PROTAC LD5097 (HY-179234) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
