2. PROTAC Apoptosis
  3. Molecular Glues Apoptosis
  4. TD-522

TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research.

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TD-522

TD-522 Chemical Structure

CAS No. : 2417647-40-4

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TD-522 Related Antibodies

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Description

TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research[1].

IC50 & Target[1]

GSPT1

0.269 nM (DC50)

In Vitro

TD-522 (0.064 nM-1 μM, 72 h) exhibits strong anti-proliferative effects in both KG-1 (EC50 = 0.5 nM) and TMD-8 (EC50 = 5.2 nM) cell lines, and shows no cytotoxic effect on VERO cells[1].
TD-522 (0.001-10 μM, 6 h) induces effectively GSPT1 degradation in a dose-dependent manner in KG1 cells, slightly degraded IKZF1 and shows no effect on CK1α[1].
TD-522 (1 μM, 3 h) significantly decreases the protein levels of GSPT1 and MYC in KG1 cells, while not affecting other IMiD’s well-known neosubstrates including IKZF1 and CK1α[1].
TD-522 displays weak hERG inhibition (IC50 = 31.6 μM) and weak inhibition of CYP 1A2, 2D6, and 3A4 at 10 μM, while exhibiting potent inhibition of CYP2C9 and 2C19[1].
TD-522 (0.001-10 μM) degrades GSPT1 and exerts its cytotoxic effects in KG-1 cells by activating the integrated stress response pathway, including the upregulation of ATF4, CHOP, and ATF3, thereby inducing apoptotic cell death[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TD-522 Related Antibodies

Western Blot Analysis[1]

Cell Line: KG-1 cells
Concentration: 0.001, 0.01, 0.1, 1 and 10 μM
Incubation Time: 6 h
Result: Degraded GSPT1 levels in a dose-dependent manner.
Caused nearly complete GSPT1 degradation (>90%) at 0.01 μM concentration.
Slightly degraded IKZF1 at 0.1 μM concentration.
In Vivo

TD-522 (50 mg/kg, i.p., daily for 14 days) suppresses tumor growth in a TMD-8 mouse xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C.B-17/IcrCrj-SCID mice injected with TMD-8B-cell lymphoma cells[1]
Dosage: 50 mg/kg
Administration: i.p., daily for 14 days
Result: Dramatically reduced tumor volume in mice.
Showed no tumor regrowth.
Showed no body weight loss during the experiment.
Molecular Weight

510.97

Formula

C25H27ClN6O4
CAS No.
SMILES

CC(C1=CC=C2N=NN(C(C2=C1)=O)C3CCC(NC3=O)=O)NC(NC4=CC=C(C(Cl)=C4)C(C)(C)C)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TD-522 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TD-5222417647-40-4TD522TD 522Molecular GluesApoptosismolecular glueGSPT1AMLDLBCLxenograftKG-1TMD-8Inhibitorinhibitorinhibit

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