2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. SD-436

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052).

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

SD-436 Chemical Structure

SD-436 Chemical Structure

CAS No. : 2497585-50-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

SD-436 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052)[1].

IC50 & Target[1]

Cereblon

 

STAT3

19 nM (IC50)

STAT1

270 nM (IC50)

STAT5

>10 μM (IC50)

STAT6

>10 μM (IC50)

In Vitro

SD-436 (4 day treatment) inhibits the growth of MOLM-16 leukemia cell line, SU-DHL-1 and SUP-M2 lymphoma cell lines, with IC50 of 0.038 μM (MOLM-16), 0.43 μM (SU-DHL-1) and 0.39 μM (SUP-M2)[1].
SD-436 (0.1 nM-40 μM, 4 or 20 h) selectively reduces the levels of STAT3 protein in human PBMCs, SU-DHL-1 and MOLM-16 cell line (4 h)[1].
SD-436 (0.1 nM-40 μM, 20 h) effectively reduces the levels of the mutated STAT3 protein (STAT3K658R) in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM[1].
SD-436 shows excellent stability in mouse, rat, dog, monkey and human plasma, with T1/2 of >120 min[1].
SD-436 has no significant inhibition of the human ether-a-go-go-related gene potassium channels (hERG inhibition: 1.3% for 3μM and 1.1% for 30 μM)[1].

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

SD-436 Related Antibodies

Western Blot Analysis[1]

Cell Line: PBMC, MOLM-16, SU-DHL-1 and Pfeiffer
Concentration: 0.1 nM, 0.5 nM, 2.5 nM, 13 nM, 64 nM, 320 nM, 1600 nM, 8000 nM, 40000 nM
Incubation Time: 20 h
Result: Reduced the levels of STAT3 protein in human PBMCs and SU-DHL-1 cell line, with DC50 of 0.1 nM and 10 nM, respectively.
Achieved near complete degradation at 320 nM with merely a 4 h treatment time in the MOLM-16 cell line.
Reduced the levels of the mutated STAT3 protein in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM.
Showed high selectivity for STAT3 over other STAT proteins.
In Vivo

SD-436 (5 mg/kg, i.v., single) effectively induces rapid, complete, and durable depletion of STAT3 in mouse native (liver and spleen) and MOLM-16 xenograft tumor tissues[1].
SD-436 (5-25 mg/kg, i.v.) shows antitumor activity in leukemia and lymphoma xenograft models in mice[1].
Pharmacokinetics of SD-436 in mice, rats, and dogs

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

Species IV dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUC(0-t) (h × ng/mL) Vz (L/kg) CI (mL/min/kg) Cl (%HBF)
ICR mouse 5 22.1 130,185 859,223 0.10 0.051 0.1%
SD rat 5 1.0 82,626 59,484 0.12 1.4 2.6%
beagle dog 1 2.3 8861 10,699 0.29 1.5 2.7%
Animal Model: MOLM-16 acute leukemia xenograft model and the SU-DHL-1 lymphoma xenograft model in SCID mice (injected subcutaneously with 3 × 106 MOLM-16 cells or 5 × 106 SU-DHL-1 cells)[1]
Dosage: 5, 10, 20 mg/kg (MOLM-16); 10, 25 mg/kg (SU-DHL-1)
Administration: Intravenous injection (i.v.); once a week, four weeks (MOLM-16: 5, 10, 20 mg/kg; SU-DHL-1: 10, 25 mg/kg) or twice a week, four weeks (SU-DHL-1: 25 mg/kg)
Result: Showed that SD-436 at 5 mg/kg was able to achieve a maximum of 76% tumor regression in the MOLM-16 leukemia xenograft model.
Induced complete tumor regression at 10 and 20 mg/kg in the MOLM-16 leukemia xenograft model.
Achieved complete and long-lasting tumor regression in the SU-DHL-1 xenograft model at 25 mg/kg weekly dosing schedule.
Molecular Weight

1248.20

Formula

C58H62F4N9O14PS
CAS No.
SMILES

O=C1[C@H](CN(CC[C@@H]2N1[C@@H](CC2)C(N[C@@H](CCC(N)=O)C(N[C@H](C(N3CCC(CC3)CCC#CC4=CC=CC5=C4CN(C5=O)C6CCC(NC6=O)=O)=O)CC7=CC=C(C(F)=C7)F)=O)=O)C(OC)=O)NC(C8=CC9=C(S8)C=CC(C(F)(P(O)(O)=O)F)=C9)=O
Shipping

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SD-436 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

SD-4362497585-50-7SD436SD 436PROTACsSTATLeukemiaLymphomaMOLM-16ICRPermeabilityXenograftInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SD-436
Cat. No.:
HY-169360
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (0 KB) Français - FR (0 KB) Deutsch - DE (0 KB) Norwegian - NO (0 KB) Español - ES (0 KB) Swedish - SV (0 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.