Catalog No.
Product Name
Application
Product Information
Citations
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PARP14 PROTAC Degrader
RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections. -
KAT2A/KAT2B PROTAC Degrader
PROTAC KAT2A/B degrader-1 is a targeted degrader that selectively induces the degradation of histone acetyltransferases KAT2A and KAT2B. This compound demonstrates significant inhibition of proliferation in acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is a valuable tool for studying the roles of KAT2A and KAT2B in cancer biology and may facilitate the development of novel therapeutic strategies for these malignancies. -
p300 PROTAC Degrader
BT-O2C is a selective p300 PROTAC degrader that effectively reduces p300 levels in HAP1 cells. It exhibits significant cytotoxicity in CIC:DUX4 sarcoma cell lines, with IC50 values ranging from 152 to 221 nM, and notably decreases the expression of target genes associated with CDS, such as ETV1, ETV4, and ETV5. This compound serves as a valuable tool for research in cancer biology, facilitating studies on p300's role in oncogenic processes. -
PCAF/GCN5 PROTAC Degrader
GSK699 is a PROTAC degrader targeting PCAF/GCN5, promoting their ubiquitination and subsequent proteasomal degradation. This compound effectively inhibits the production of key cytokines and chemokines, such as interleukin-6 (IL-6) and CXCL1/GROα, thus demonstrating significant anti-inflammatory properties. GSK699 is suitable for investigations related to inflammatory diseases and other conditions modulated by these target proteins. -
BRD4/CBP/p300 PROTAC Degrader
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer. -
ATR PROTAC Degrader
PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia. -
SIRT6 PROTAC Degrader
SZU-B6 is a SIRT6-protein-targeting chimeric degrader that achieves a DC50 of 45 nM and 154 nM in SK-HEP-1 and Huh-7 cell lines, respectively. It effectively inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cells. Additionally, SZU-B6 induces apoptosis and causes a cell cycle arrest in the G2/M phase in SK-HEP-1 cells, demonstrating notable antitumor efficacy in mouse models. This compound serves as a valuable tool for studying the functional roles of SIRT6 in cancer research. -
SMARCA2 Degrader
A947 is a selective SMARCA2 proteolysis-targeting chimera (PROTAC) that functions as a potent degrader of SMARCA2. It exhibits a binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM, establishing its effectiveness in mediating targeted protein degradation. This compound has significant applications in cancer research, facilitating studies on the role of SMARCA2 in tumorigenesis and potential therapeutic interventions. -
HCK/BTK PROTAC Degrader
DFCI-002-06 is an orally active PROTAC degrader targeting both HCK and BTK, demonstrating DC₅₀ values of 1.3 nM and 4.5 nM, respectively. This compound exhibits superior anti-tumor activity compared to a dual-target inhibitor, promoting apoptosis in cancer cells, particularly in MYD88 mutant B-cell malignancies. DFCI-002-06 serves as a valuable tool for researching mechanisms underlying these specific cancer types. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-17 is a potent protein degrader targeting bromodomain-containing protein 4 (BRD4). It exhibits IC50 values of 29.54 nM for BRD4 (BD1) and 3.82 nM for BRD4 (BD2). This compound effectively inhibits G2/M cell cycle progression, leading to decreased expression of Cyclin B1, and significantly induces apoptosis in MV-4-11 cells. PROTAC BRD4 Degrader-17 is valuable for research applications focused on cancer cell biology and the development of targeted degraders in therapeutic strategies. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 5 is a targeted protein degradation agent that effectively degrades the EGFRDel19 variant in HCC827 cells, exhibiting a DC50 of 34.8 nM. This compound significantly induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells, making it a valuable tool for studying EGFR-related signaling pathways and potential therapeutic interventions in lung cancer research. -
FLT3-PROTAC Degrader
PROTAC FLT-3 degrader 4 is a CRBN-based degrader that selectively targets FLT3-ITD mutants by harnessing the ubiquitin-proteasome system for degradation. This compound demonstrates potent activity against FLT3-ITD mutant acute myeloid leukemia (AML) cells, offering a focused approach for research applications in cancer therapeutics. Its oral bioavailability positions it as a valuable tool for investigating FLT3-related signaling pathways and potential treatment strategies in AML. -
p53 Stabilizer/MDM2 PROTAC Degrader
Seldegamadlin is a selective p53 stabilizer and an MDM2 PROTAC degrader with a DC50 of 0.4 nM. It effectively inhibits the proliferation of RS4;11 cancer cells, demonstrating an IC50 of 0.3 nM, and induces cell cycle arrest at the G2/M phase while promoting apoptosis. By upregulating p53 activity, Seldegamadlin overcomes the p53-MDM2 feedback loop, making it a valuable tool for research in hematologic and solid tumors, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). -
AR-FL/AR-V7 PROTAC Degrader
BWA-522 is an orally active PROTAC degrader that targets the full-length androgen receptor (AR-FL) and its splice variant AR-V7. By antagonizing the N-terminal domain of the androgen receptor, BWA-522 effectively suppresses downstream signaling pathways and induces apoptosis in cancer cells. Furthermore, this compound has demonstrated significant inhibition of tumor growth in LNCaP xenograft mouse models, making it a valuable tool for prostate cancer research. -
CDK4/6 PROTAC Degrader
PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies. -
CCND1/CDK4 PROTAC Degrader
CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 9 is a CRBN-based PROTAC designed to specifically target and degrade the mutant forms of the epidermal growth factor receptor (EGFR), particularly EGFRL858R/T790M/C797S. It demonstrates potent degradation activity with a DC50 of 10.2 nM and a Kd of 240.2 nM, effectively eliminating EGFR mutants while leaving wild-type EGFR unaffected. This compound serves as a valuable tool in cancer research, particularly in studies focused on targeted therapies for EGFR-driven malignancies. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer. -
PROTAC CDK4/6 degrader
HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology. -
PROTAC ERα Degrader
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies. -
PROTAC HDAC8 Degrader
SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation. -
PROTAC eEF2K Degrader
PROTAC eEF2K degrader-1 is a small molecule designed to target and induce degradation of the elongation factor 2 kinase (eEF2K). This compound has been shown to effectively promote apoptosis in MDA-MB-231 cancer cells, demonstrating its potential in cancer research. The mechanism of action involves the targeted elimination of eEF2K, providing a valuable tool for studying the role of this kinase in cellular processes and therapeutic applications. -
PROTAC XPO1 Degrader
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. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4 degrader-38 is a dual-targeted PROTAC degrader designed to promote the ubiquitination and subsequent degradation of the SMARCA2 and SMARCA4 proteins. With DC50 values of 3.0 nM and 4.0 nM for SMARCA2 and SMARCA4 respectively, this compound effectively blocks the G0/G1 cell cycle phase and induces apoptosis in cancer cells. It has significant potential for use in research focused on acute myeloid leukemia (AML) and other malignancies involving these chromatin remodeling factors. -
PROTAC JAK2 Degrader
SJ1008030 is a PROTAC compound designed to selectively degrade Janus kinase 2 (JAK2). This compound exhibits potent inhibitory activity against MHH–CALL-4 cell growth, with an IC50 of 5.4 nM. SJ1008030 is valuable for research applications focusing on leukemia, facilitating the study of JAK2-related pathways and therapeutic interventions. -
PROTAC FLT3/JAK2/BRD4 Degrader
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML). -
PROTAC FGFR1/2 Degrader
DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies. -
BCR-ABL PROTAC Degrader
Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy. -
BCR-Abl PROTAC Degrader
GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development. -
mini-PROTAC BCR-ABL Degrader
Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies. -
PROTAC degrader
P19As is a PROTAC degrader that targets the BCR-ABL fusion protein, exhibiting a DC50 value of approximately 200 nM for wild-type BCR-ABL. This compound effectively degrades the T315I mutant variant and demonstrates potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cell lines. P19As serves as a valuable tool for investigating therapeutic strategies in chronic myeloid leukemia and acute lymphoblastic leukemia. -
BCR-ABL PROTAC Degrader
P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells. -
BCR-ABL PROTAC Degrader
SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML. -
BCR-ABL PROTAC Degrader
SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia. -
BCR-ABL PROTAC Degrader
P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies. -
BCR-ABL PROTAC Degrader
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies. -
PROTAC FLT3-ITD Degrader
PF15 is a PROTAC designed to target FLT3 kinase through its ligands linked with CRBN. This highly selective FLT3-ITD degrader exhibits a DC50 of 76.7 nM, effectively inhibiting the proliferation of FLT3-ITD-positive cells. PF15 down-regulates the phosphorylation of FLT3 and STAT5, demonstrating significant anti-tumor activity in mouse models, making it a valuable tool for leukemia research. -
LCK PROTAC Degrader
SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia. -
PROTAC CDK4/6/9 Degrader
PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype. -
PROTAC USP7 Degrader
XM-U-14 is a selective PROTAC degrader targeting USP7, demonstrating a DC50 of 0.74 nM for inducing USP7 degradation in the RS4;11 cell line. This compound effectively upregulates p53 and p21 levels and exhibits significant inhibition of acute lymphoblastic leukemia (ALL) cell proliferation, with IC50 values of 0.5 nM and 8.3 nM for RS4;11 and Reh cells, respectively. Additionally, XM-U-14 induces apoptosis and cell cycle arrest, ultimately inhibiting tumor growth, making it a valuable tool for cancer research and therapeutic exploration. -
RET PROTAC Degrader
RD-23 is a selective RET PROTAC degrader that functions through the promotion of ubiquitination and subsequent degradation of the RETG810C mutation, exhibiting a DC50 value of 11.7 nM. This compound effectively inhibits downstream Shc signaling pathways and induces apoptosis in RET-related cancer models. RD-23 is a valuable tool for investigating the biological roles and therapeutic targeting of RET in oncology research. -
EML4-ALK PROTAC Degrader
Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments. -
AR PROTAC Degrader
ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer. -
BRD4 PROTAC Degrader
NEP162 is a potent BRD4 PROTAC degrader, demonstrating DC50 values of 1.2 and 1.6 μM in SW480 and U2OS cell lines, respectively. It exhibits significant antiproliferative activity, effectively inhibiting tumor growth and promoting apoptosis in various cancer models. NEP162 is particularly relevant for research applications in osteosarcoma, colorectal cancer, and non-small cell lung cancer. -
AR PROTAC degrader
PROTAC AR-NTD degrader 1 is a protein-targeting chimera designed to selectively target and degrade the N-terminal domain of the Androgen Receptor (AR-V7). This small molecule exhibits significant efficacy in inducing apoptosis in prostate cancer cells, demonstrating a degradation efficiency of 62.2% at 1 μM and 71.1% at 5 μM in VCaP cells. PROTAC AR-NTD degrader 1 is a valuable tool for research focused on androgen receptor signaling and its implications in prostate cancer therapy. -
PROTAC IRAK4 Degrader
KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research. -
HDAC1-3 PROTAC Degrader
JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-16 is an effective degrader specifically targeting BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). This compound is known to significantly reduce Cyclin B1 expression, which is associated with G2/M cell cycle progression. Additionally, PROTAC BRD4 Degrader-16 effectively induces apoptosis in MV-4-11 cells, contributing to its potential utility in cancer research and therapeutic applications. -
Bcr-AblT315 PROTAC Degrader
PROTAC BCR-ABL Degrader-2 is a selective degrader targeting the Bcr-AblT315 mutant, with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. This compound demonstrates a notable degradation efficacy, achieving degradation rates of 69.89% and 94.23% at concentrations of 100 nM and 300 nM, respectively. Additionally, it shows promising in vivo anti-tumor effects including significant tumor regression and induction of apoptosis in tumor cells, while maintaining a favorable safety profile. PROTAC BCR-ABL Degrader-2 is suitable for research focused on chronic myeloid leukemia (CML). -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 6 is a selective degrader targeting the EGFRDel19 mutant, exhibiting a DC50 value of 45.2 nM in HCC827 cells. This compound effectively induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells. Its unique mechanism of action makes it a valuable tool for research focused on EGFR-related pathways and the development of targeted cancer therapies.
