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antiproliferative

" in TargetMol Product Catalog
  • Inhibitors & Agonists
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Thailanstatin A
T388891426953-21-0
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.
  • $187
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TargetMol | Inhibitor Hot
BSJ-4-116
T91172519823-34-6
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
  • $50
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PROTAC METTL3 degrader 1
T200771
PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based degrader of METTL3, demonstrating a DC50 of 220 nM in MOLM-13 cells. This compound inhibits the METTL3 14 complex with an IC50 of 341 nM and exhibits antiproliferative activity against AML cells.
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PROTAC SMARCA2 degrader-31
T2008532380274-45-1
PROTAC SMARCA2-degrader-36 (compound 38) is an SMARCA2 degrader that achieves a 99% degradation rate at 100 nM in H929 cells. It possesses antiproliferative activity and is used in cancer research.
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PROTAC SMARCA2 degrader-26
T2011432760247-27-4
PROTAC SMARCA2 degrader-26 (compound 45) is an effective degrader of SMARCA2 using the PROTAC technology. It induces degradation of SMARCA2 and SMARCA4 in VCaP cells, with degradation percentages of 94% and 57%, respectively. Additionally, PROTAC SMARCA2 degrader-26 demonstrates antiproliferative activity.
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CQ-16
T2015403024354-59-1
CQ-16 is an orally active small molecule drug conjugate (SMDC) that targets prostate-specific membrane antigen (PSMA). It exhibits high selectivity in its antiproliferative activity between PSMA-positive and PSMA-negative prostate cells. Additionally, CQ-16 possesses PARP inhibitory activity (IC50=1 nM).
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CPD-10
T2015773055471-57-0
CPD-10 is a potent bifunctional PROTAC degrader targeting CCND1 and CDK4 and exhibits antiproliferative effects. It induces apoptosis and reduces the protein expression of Cyclin D1, Cyclin D3, CDK4, and P-Rb(5807 811) in a dose-dependent manner.
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CSI86
T201659
CSI86 is a PROTAC degrader targeting MYC, exhibiting antiproliferative activity (IC50: 13-18 μM).
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CPD-39
T2017363055472-38-0
CPD-39 is an efficacious and orally active bifunctional PROTAC degrader targeting both CCND1 and CDK4. It exhibits antiproliferative effects.
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BTX6654
BTX-6654, BTX 6654
T203787
BTX-6654 is a cereblon-based bifunctional SOS1 PROTAC degrader. This compound exhibits antiproliferative activity against cells with various KRAS mutations by reducing the expression of downstream signaling markers pERK and pS6.
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YB-3–17
T2041112940242-88-4
YB-3-17 is a bifunctional molecule that can inhibit mTOR with an IC50 of 0.22 nM or degrade the G1 to S phase transition 1 gene (GSPT1) through the PROTAC mechanism, with a DC50 of 5 nM. It exhibits antiproliferative activity at nanomolar concentrations in various glioblastoma cell lines. Additionally, YB-3-17 shows antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)
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PROTAC SMARCA2/4 degrader-36
T2042813033588-00-7
PROTACSMARCA2 4 degrader-36 (Compound 29) is a potent dual degrader targeting SMARCA2 and SMARCA4, exhibiting DC50 values of 0.22 nM and 0.85 nM, respectively. Additionally, PROTACSMARCA2 4 degrader-36 demonstrates antiproliferative activity.
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HGC652
T2046703055558-98-7
HGC652 is a molecular glue that targets the E3 ubiquitin ligase TRIM21, facilitating the formation of a ternary complex between TRIM21 and NUP98, which induces the degradation of NUP155 and nuclear pore complex proteins, ultimately leading to cell death. HGC652 inhibits the proliferation of various cancer cells, with its antiproliferative activity depending on the expression level of TRIM21.
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CQ627
T204921
CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2 M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.
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QXG-6442
T205020
QXG-6442 is a molecular glue degrader targeting CK1α, demonstrating a degradation potency with a DC50 of 5.7 nM and a Dmax of 90%. In the MOLM-14 cell line, QXG-6442 induces antiproliferative effects.
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DP-15
T2050433033837-71-4
DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]
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E3 Ligase Ligand-linker Conjugate 170
T2051902379572-21-9
E3 Ligase Ligand-linker Conjugate 170 (Compound I) demonstrates antiproliferative activity in non-Hodgkin's lymphoma SU-DHL-4 cells, with an IC50 of less than 0.2 μM. This conjugate is composed of an E3 ligase ligand and a linker, making it suitable for use in PROTAC synthesis.
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dBRD9 HCl
dBRD9 HCl(2170679-45-3 Free base)
T31221L2341840-98-8
dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.
  • $197
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MIF degrader MD13
T695252758431-97-7
MIF degrader MD13 is involved in protein-protein interactions that play key roles in inflammation and cancer. Current strategies to develop small molecule modulators of MIF functions are mainly restricted to the MIF tautomerase active siteMIF degrader MD13. MD13 also exhibits antiproliferative effect in a 3D tumor spheroid model. In conclusion, we describe the first MIF-directed PROTAC (MD13) as a research tool, which also demonstrates the potential of PROTACs in cancer therapy.
  • TBD
35 days
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protac brd9-binding moiety 5
T74256893633-37-9
PROTAC BRD9-binding moiety 5, a selective binder of BRD9 with an IC50 value of 4.20 μM, is utilized in PROTAC synthesis and exhibits antiproliferative activity against cancer cells [1].
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FAK PROTAC B5
T742812471525-44-5
Compound B5 (FAK PROTAC B5) is a FAK PROTAC degrader exhibiting potent FAK degradation and antiproliferative activities, with an IC50 of 14.9 nM. It also shows excellent plasma stability, moderate membrane permeability, and inhibits cell migration and invasion [1].
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protac egfr degrader 2
T74333
PROTAC EGFR degrader 2 is a potent compound with an IC50 of 4.0 nM, demonstrating strong antiproliferative activity, and a DC50 of 36.51 nM, indicating robust EGFR degradation activity. It is suitable for synthesizing nitroreductase (NTR)-responsive PROTACs [1].
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PP-C8
T74359
PP-C8, a potent and selective PROTAC CDK12-Cyclin K degrader, efficiently induces degradation of CDK12 and Cyclin K, with DC50 values of 416 nM and 412 nM, respectively. This compound exhibits significant synergistic antiproliferative effects when combined with a PARP inhibitor in triple-negative breast cancer (TNBC) [1].
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PROTAC SOS1 degrader-1
T744392913185-35-8
PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].
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