Art. -Nr.: HY-149924

CST626

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CST626 is a PROTAC degrader targeting IAP, with DC₅₀ values of 0.7 nM, 2.4 nM and 6.2 nM against XIAP, cIAP1 and cIAP2, respectively. This compound recruits the VHL E3 ubiquitin ligase to form a heterotrimeric complex, thereby inducing ubiquitination and proteasomal degradation of the target proteins. CST626 also exhibits certain degrading activity against VHL30 and VHL19. CST626 inhibits the proliferation and induces apoptosis of various hematologic tumor cell lines, and its anti-tumor effect is further enhanced when used in combination with TNF-α. CST626 can be used in research related to multiple myeloma, acute myeloid leukemia and diffuse large B-cell lymphoma.
(Pink: IAP and XIAP ligand (HY-175925); Blue: VHL ligand (HY-112078); Black: linker).

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Reinheit: 99.60%
CAS. Nr.: 3033993-13-1
Formel: C₆₁H₈₂N₈O₉S
Molecular Weight:1103.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CST626 Chemical Structure

CAS. Nr.: 3033993-13-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CST626 is a PROTAC degrader targeting IAP, with DC₅₀ values of 0.7 nM, 2.4 nM and 6.2 nM against XIAP, cIAP1 and cIAP2, respectively. This compound recruits the VHL E3 ubiquitin ligase to form a heterotrimeric complex, thereby inducing ubiquitination and proteasomal degradation of the target proteins. CST626 also exhibits certain degrading activity against VHL30 and VHL19. CST626 inhibits the proliferation and induces apoptosis of various hematologic tumor cell lines, and its anti-tumor effect is further enhanced when used in combination with TNF-α. CST626 can be used in research related to multiple myeloma, acute myeloid leukemia and diffuse large B-cell lymphoma^[1]^[2]. (Pink: IAP and XIAP ligand (HY-175925); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target^[1]

XIAP

0.7 nM (EC₅₀)

cIAP1

2.4 nM (EC₅₀)

cIAP2

6.2 nM (EC₅₀)

VHL30

VHL19

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle IAP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
DB	IC₅₀	0.46 μM Compound: 9; CST626	Cytotoxicity against human DB cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human DB cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
HEL	IC₅₀	1.17 μM Compound: 9; CST626	Cytotoxicity against human HEL cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human HEL cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
JJN-3	IC₅₀	1.14 μM Compound: 9; CST626	Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
K562	IC₅₀	0.42 μM Compound: 9; CST626	Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
MOLM-13	IC₅₀	0.002 μM Compound: 9; CST626	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
NCI-H929	IC₅₀	0.008 μM Compound: 9; CST626	Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
RPMI-8226	IC₅₀	2.54 μM Compound: 9; CST626	Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
SUD4	IC₅₀	1.69 μM Compound: 9; CST626	Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
SU-DHL-6	IC₅₀	0.001 μM Compound: 9; CST626	Cytotoxicity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]

In Vitro

CST626 (0.0001-1 μM; 16 h) potently induces pan-IAP degradation in MM.1S cells with DC₅₀ values of 0.7 nM (XIAP), 2.4 nM (cIAP1), and 6.2 nM (cIAP2), and also degrades VHL isoforms^[1].
CST626 (0.1 μM; 3-6 h) induces complete degradation of cIAP1, cIAP2, and XIAP in MM.1S cells within 3 h at 0.1 μM, with maximal VHL30 degradation observed at 6 h^[1].
CST626 (1 μM; single exposure, followed by incubation up to 72 h post-washout) mediates long-lasting pan-IAP degradation in MM.1S cells for up to 72 h after a single 1 μM exposure, while VHL isoform levels recover more quickly^[1].
CST626-induced IAP degradation in MM.1S cells relies on the functional ubiquitin-proteasome system^[1].
CST626 (0.1 μM; 3 h) selectively degrades cIAP1 and XIAP in MM.1S cells at 0.1 μM after 3 h, with no significant off-target proteome-wide effects^[1].
CST626 (0.0016-10 μM; 96 h) potently inhibits viability of multiple hematological cancer cell lines under TNF-α-challenged conditions, with IC₅₀ values ranging from 0.0016 μM (SUDHL6) to 2.54 μM (RPMI-8226), and shows superior activity compared to IAP antagonists in select cell lines^[1].
Combination of VenAza with CST626 (100 nM) significantly increases cytotoxicity in TP53^+/+ and TP53^-/R248Q MOLM-13 AML cells compared to VenAza or CST626 alone^[2].
CST626 (100-200 nM) induces apoptosis in TP53^+/+, TP53^-/R248Q, and TP53^-/- MOLM-13 AML cells, with greater apoptosis observed at the 200 nM concentration compared to 100 nM^[2].

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

Western Blot Analysis^[1]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

0.001, 0.01, 0.1, 1 μM
Incubation Time:

16 h
Result:

Induced dose-dependent degradation of cIAP1, cIAP2, XIAP, VHL30, and VHL19.
Reached DC₅₀ values of 2.4 nM for cIAP1, 6.2 nM for cIAP2, and 0.7 nM for XIAP.
Achieved maximum degradation (Dmax) of >99% for cIAP1 and XIAP, and >90% for cIAP2 at 0.1 μM.

Western Blot Analysis^[1]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

0.1 μM
Incubation Time:

3, 6, 24, 48, 72, 96 h
Result:

Induced complete degradation of cIAP1, cIAP2, and XIAP after 3 h of treatment.
Detected the most pronounced depletion of VHL30 after 6 h of treatment.

Western Blot Analysis^[1]

Cell Line:

MM.1S multiple myeloma cells
Concentration:

1 μM
Incubation Time:

2, 5, 8, 24, 48, 72 h
Result:

Maintained nearly full and stable pan-degradation of cIAP1, cIAP2, and XIAP up to 72 h post-washout.
Restored VHL19 and VHL30 levels more rapidly after compound removal.

Cell Viability Assay^[1]

Cell Line:

nine hematological cancer cell lines (RPMI-8226, JJN3, NCI-H929, HEL, K562, MOLM13, SUDHL4, DB, SUDHL6)
Concentration:

0.001, 0.01,0.1, 0.4, 1, 4, 10 μM
Incubation Time:

96 h
Result:

Inhibited cell viability with IC₅₀ values of 2.54 μM (RPMI-8226), 1.14 μM (JJN3), 0.0085 μM (NCI-H929), 1.17 μM (HEL), 0.42 μM (K562), 0.0021 μM (MOLM13), 1.69 μM (SUDHL4), 0.46 μM (DB), and 0.0016 μM (SUDHL6).
Outperformed IAP antagonists in several cell lines, including NCI-H929, MOLM13, and SUDHL6.

Chemical Information

CAS. Nr. 3033993-13-1
Appearance Solid
Molecular Weight 1103.42
Formel C₆₁H₈₂N₈O₉S
Color White to off-white
SMILES

O=C([C@H]1N(C([C@H](C2CCCCC2)NC([C@@H](NC)C)=O)=O)C[C@@H](OC3=CC=CC(OCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)=C3)C1)N[C@@H]7CCCC8=C7C=CC=C8
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (90.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9063 mL

4.5314 mL

9.0627 mL

5 mM

0.1813 mL

0.9063 mL

1.8125 mL

10 mM

0.0906 mL

0.4531 mL

0.9063 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (2.27 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (2.27 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (2.27 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ng YLD, et al. Heterobifunctional Ligase Recruiters Enable pan-Degradation of Inhibitor of Apoptosis Proteins. Journal of medicinal chemistry. 2023 Apr 13;66(7):4703-4733. [Content Brief]

[2]. Mamdouh AM, et al. Targetable BIRC5 dependency in therapy-resistant TP53 mutated acute myeloid leukemia. bioRxiv [Preprint]. 2025 May 22:2025.05.17.654633. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	0.9063 mL	4.5314 mL	9.0627 mL	22.6568 mL
	5 mM	0.1813 mL	0.9063 mL	1.8125 mL	4.5314 mL
	10 mM	0.0906 mL	0.4531 mL	0.9063 mL	2.2657 mL
	15 mM	0.0604 mL	0.3021 mL	0.6042 mL	1.5105 mL
	20 mM	0.0453 mL	0.2266 mL	0.4531 mL	1.1328 mL
	25 mM	0.0363 mL	0.1813 mL	0.3625 mL	0.9063 mL
	30 mM	0.0302 mL	0.1510 mL	0.3021 mL	0.7552 mL
	40 mM	0.0227 mL	0.1133 mL	0.2266 mL	0.5664 mL
	50 mM	0.0181 mL	0.0906 mL	0.1813 mL	0.4531 mL
	60 mM	0.0151 mL	0.0755 mL	0.1510 mL	0.3776 mL
	80 mM	0.0113 mL	0.0566 mL	0.1133 mL	0.2832 mL

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CST626

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle IAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CST626 Related Classifications

HY-149924 Related Classifications