2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. Molecular Glues STAT
  4. KT-333

KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

For research use only. We do not sell to patients.

KT-333 Chemical Structure

KT-333 Chemical Structure

CAS No. : 2502186-79-8

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Based on 1 publication(s) in Google Scholar

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Description

KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL)[1].

IC50 & Target[1]

STAT3

 

In Vitro

KT-333 (11.8±2.3 nM, 48 h) degrades STAT3 resulted in irreversible growth inhibition of SU-DHL-1 cell line and induces caspase 3/7 activity in the SU-DHL-1 cell line[1].
KT-333 has a good degradation effect on STAT3 protein, and in cell phenotypic analysis, its GI50 value in multiple ALCL cell lines ranges from 8.1 to 57.4 nM[1].

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

KT-333 Related Antibodies
In Vivo

KT-333 (5, 10, 15 and 45 mg/kg, iv.; once a week for two weeks) exhibits dose-dependent antitumor activity. Female NOD SCID mice with xenograft tumors of SU-DHL-1 administered with 5 mg/kg achieved 79.9% tumor growth inhibition (TGI), while those administered 10, 15, or 45 mg/kg experienced complete tumor regression, with these effects sustained until the end of the study[1].
KT-333 (10, 20 and 30 mg/kg, iv.; once a week for two weeks) exhibits dose-dependent antitumor activity. Female NOD SCID mice with xenograft tumors of SUP-M2 administered with 10 mg/kg achieved 83.8% tumor growth inhibition (TGI), while those administered 20 or 30 mg/kg experienced complete tumor regression, with these effects sustained until the end of the study[1].

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

1257.78

Formula

C60H74ClN10O14PS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@H](C2)NC(C3=CC4=CC(C([P](O)(O)=O)=O)=CC=C4N3)=O)=O)[C@](CCN2C(C)=O)([H])CC1)N[C@@H](CCC(N)=O)COC(C=CC=C5CCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H]6O)[C@@H](C6)C(N[C@H](C7=CC=C(C(SC=N8)=C8C)C=C7)C)=O)=O)=O)=C5Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (99.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7951 mL 3.9753 mL 7.9505 mL
5 mM 0.1590 mL 0.7951 mL 1.5901 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.7951 mL 3.9753 mL 7.9505 mL 19.8763 mL
5 mM 0.1590 mL 0.7951 mL 1.5901 mL 3.9753 mL
10 mM 0.0795 mL 0.3975 mL 0.7951 mL 1.9876 mL
15 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3251 mL
20 mM 0.0398 mL 0.1988 mL 0.3975 mL 0.9938 mL
25 mM 0.0318 mL 0.1590 mL 0.3180 mL 0.7951 mL
30 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6625 mL
40 mM 0.0199 mL 0.0994 mL 0.1988 mL 0.4969 mL
50 mM 0.0159 mL 0.0795 mL 0.1590 mL 0.3975 mL
60 mM 0.0133 mL 0.0663 mL 0.1325 mL 0.3313 mL
80 mM 0.0099 mL 0.0497 mL 0.0994 mL 0.2485 mL
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KT-333 Related Classifications

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:

KT-3332502186-79-8KT333KT 333Molecular GluesSTATMolecular gluessmall molecule degradationSTAT3SU-DHL-1 cell lineSUP-M2 cell lineInhibitorinhibitorinhibit

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