An E3 ligase ligand-linker conjugate for PROTAC..

Pomalidomide-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.

TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide.

dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..

N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

Pomalidomide 4'-alkylC5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.

Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.

Thalidomide-O-C4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

GK420 (AVX420) is a potent inhibitor of cytosolic phospholipase A2α (cPLA2α), with the XI(50) of 0.0016. GK420 inhibits arachidonic acid release with the EC50 of 0.09 μM. GK420 plays an important role in cancer research.

Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs.

S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.

AZD2716(AZD-2716) is a novel potent, selective, orally bioavailable sPLA2 inhibitor with excellent plasma sPLA2 inhibition (IC50=0.1 nM).

SC-919 (SC919) is a potent, selective inhibitor of IP6K (Inositol hexakisphosphate kinase) with IC50 of <5.2, <3.8 and 0.65 nM for human IP6K1/2/3, respectively.

JPH203 (KYT-0353) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2.

JPH203, also known as KYT-0353, is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic Y

SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.

RMC-6236 (Compound A122) is a potent RAS(ON)MULTI inhibitor and can be used for the research of cancer.

Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 blocked nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants, including G12A/C/D/F/V/S, G13C/D, V14I, L19F, Q22K, D33E, Q61H, K117N and A146V/T. Inhibition of downstream signalling and proliferation was restricted to cancer cells harbouring mutant KRAS, and drug treatment suppressed KRAS mutant tumour growth in mice, without having a detrimental effect on animal weight.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

A broad-spectrum natural antifungal compound that acts as a selective and highly potent fungal Pkc1 kinase inhibitor.

HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.

Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irritable bowel syndrome.

Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1).

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant in combination with a HER2 inhibitor, works on ER+/HER2+ cancer.

CP 94253 hydrochloride is a potent and selective serotonin 5-HT1B receptor agonist, with Ki values to be 2 nM for 5-HT1B and 89, 860, 49 and 1600 nM for 5-HT1A, 5-HT1C, 5-HT1D and 5-HT2 receptors respectively.

TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.

Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM).

NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research.