Protein Degradation & Proteostasis

dBET6

CAS 1950634-92-0

dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.

2-(Aminooxy)ethanamine dihydrochloride

CAS 3633-17-8

2-(Aminooxy)ethanamine (dihydrochloride) is a PROTAC linker that can be used in the synthesis of PROTACs.

XY028-140 (MS140)

CAS 2229974-83-6

XY028-140 (MS140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its…

NJH-2-075

NJH-2-075 is an alkyne-functionalized probe of EN523, retains binding to OTUB1 in vitro.

ARV-766

CAS 2750830-09-0

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].

MS934

CAS 2756323-15-4

MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in…

ErSO

CAS 2407860-35-7

ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.

AGB1

CAS 2776190-62-4

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary affinity to VHL (Kd=125 nM). AGB1 exhibits…

SJ3149

CAS 3026986-17-1

SJ3149 is a uniquely potent and selective CK1α degrader with DC50 of 3.7 nM. SJ3149 shows high activity across a range of acute leukemia (AL) cell lines derived from different hematologic neoplasms, such as B-cell and T-cell acute lymphoblastic leukemia.…

Suramin sodium salt

CAS 129-46-4

Suramin sodium salt (BAY-205, NF-060) is an antitrypansomal drug that also possesses antitumor activity; inhibits CRL (Cullin-RING E3 ubiquitin ligases) activity by disrupting its ability to recruit Cdc34; induces accumulation of CRL substrates; also inhi

Vepdegestrant (ARV-471)

CAS 2229711-68-4

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

amyloid P-IN-1(GSK3039294)

CAS 1819986-22-5

pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and…

Leupeptin hemisulfate

CAS 103476-89-7

Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor, which has been shown to inhibit cathepsins B, H, L, and S, calpain, and trypsin. Leupeptin hemisulfate is an orally active, antioxidant and anti-inflammatory agent.

PT-179

CAS 2924858-25-1

PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.

HA-9104

CAS 2412367-83-8

HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.

ARV-393

CAS 2851885-95-3

ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC50 and GI50 values of <1 nM in…

(R)-CR8

CAS 294646-77-8

(R)-CR8 (CR8), a second-generation derivative of Roscovitine, is a highly effective inhibitor of CDK1/2/5/7/9. It exhibits inhibitory activity against CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM),…

Tunicamycin

CAS 11089-65-9

Antibiotic, inhibiting the first step in the N-linked glycosylation in eukaryotes and inducing ER stress to activate the unfolded protein response (UPR)

Shield-1

CAS 914805-33-7

Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entire…

5M-8OH-Q

CAS 312611-90-8

5M-8OH-Q is a specific small molecule inhibitor of UDP-glucose glycoprotein glucosyltransferase (UGGT), binds a CtUGGTGT24 “WY” conserved surface motif conserved across UGGTs (Kd=47 uM) but not present in other GT24 family glycosyltransferases.

17-AAG

CAS 75747-14-7

17-AAG is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90.

Geldanamycin (NSC122750)

CAS 30562-34-6

Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry…

MG-132

CAS 133407-82-6

MG-132 is a potent, reversible, and cell-permeable 20S proteasome inhibitor which inhibits proteasomal chymotrypsin-like peptidase activity with an IC50 of 24.2 nM.

NSC112200

CAS 28293-38-1

NSC112200 is a chemical inhibitor of the EZH2 deubiquitinase ZRANB1 (at 10 uM), destabilizes EZH2, promotes proteasomal degradation of EZH2 and inhibits the viability of TNBC cells; NSC112200 is a mixture of 2,5-dibromo-3,6-dimethyl-1,4- benzenediol and…

ACBI3

CAS 2938169-76-5

ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).

XL177A

CAS 2417089-74-6

XL177A is a potent USP7 inhibitor. XL177A irreversibly inhibits USP7 with sub-nM potency and selectivity across the human proteome. Evaluation of the cellular effects of XL177A reveals that selective USP7 inhibition suppresses cancer cell growth predominantly…

MS8815

CAS 2855085-25-3

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).

ADAM9i

CAS 860786-85-2

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

MRT6160

CAS 3050683-38-7

MRT-6160 represents a groundbreaking molecular glue degrader designed to selectively target VAV1, achieving its proteasomal degradation with a DC50 value of 7 nM. This innovative compound showcases its unique mechanism and therapeutic potential.

Luteolin 7-O-glucuronide (Luteolin 7-glucuronide4)

CAS 29741-10-4

Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.

SKPer1 (XMU-MP-8)

SKPer1 (XMU-MP-8) is a small-molecule degrader of SKP2 that triggers degradation of the oncoprotein SKP2 and specifically kills SKP2-expressing cancer cells.

HY041004

CAS 2412899-25-1

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.

Carfilzomib (PR-171)

CAS 868540-17-4

Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

Erdafitinib

CAS 1346242-81-6

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

CCF642

CAS 346640-08-2

CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.The IC50 is 2.9 μmol/L.

Tri-GalNAc-β-Ala-PEG3-MAL

Tri-b-GalNAc-b-Ala-PEG3-MAL contains three terminal beta-N-acetylgalactosamine (GalNAc) sugars arranged in a trivalent configuration, facilitating high-affinity binding to the asialoglycoprotein receptor (ASGPR) expressed on hepatocyte surfaces. The crucial…

(+)-JQ1 carboxylic acid

CAS 202592-23-2

JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.

E3 Ligase Ligand-Linker Conjugates 22

CAS 2225940-52-1

E3 Ligase Ligand-Linker Conjugates 22 incorporates an E3 ligase ligand and a linker, can be used for the treatment of EZH2-mediated cancer.

STF-083010

CAS 307543-71-1

STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

Batimastat(BB-94)

CAS 130370-60-4

Batimastat is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

MG115

CAS 133407-86-0

MG-115(MG 115) is an inhibitor of NFκB in the cytoplasm by acting on IKK or the proteasome.

AK778

CAS 328906-67-8

AK778 (Col001) is a small-molecule compound that inhibits the interaction of Hsp47 with collagen, competitively inhibits the interaction and causes the inhibition of collagen secretion by destabilizing the collagen triple helix.

Thalidomide-5-OH

CAS 64567-60-8

Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs[1].

MID-1

CAS 312608-54-1

MID-1 is an inhibitor of MG53-IRS-1 (Mitsugumin 53-Insulin Receptor Substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1…

STD1T

CAS 893075-58-6

STD1T (USP2a inhibitor STD1T) is a hit-to-lead, small-molecule inhibitor of USP2a with IC50 of 3.3 uM in Ub-AMC assays, displays no activity against USP7 at 10 uM.

SJ6986

CAS 2765625-93-0

SJ6986 is a highly potent, selective, and orally bioavailable degrader of GSPT1/2, with a DC50 of 2.1 nM. It exhibits strong antiproliferative effects in MV4-11 and MHH-CALL-4 cell lines, showing IC50 values of 1.5 nM and 0.4 nM, respectively.

NRX2663

CAS 2763260-34-8

NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM1.

SZL P1-41

CAS 222716-34-9

SZL P1-41 is Skp2 inhibitor, selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes.